Ustinova Yu. V.   Borodulin D. M.   and Donya D. V.   

The results of experimental studies on the effect of shungite crushed stone on the therapeutic mineral waters of the sanatorium "Belokurikha" (Altai), used for the treatment of complex chronic diseases, are presented. The experiment was carried out using various samples of mineral waters pretreated with a natural mineral – shungite (Karelia), which includes fullerene C₆₀, which is a special allotropic molecular modification of carbon. Samples of artificial and natural shungite water were taken as comparison samples. It has been established that the main sensitive indicator of the quality of the studied water systems is their redox potential. Two possible mechanisms of action of fullerenes on mineral waters are presented. The fact of accelerated decay of residual radiation of radionuclides in the presence of fullerene, which performs the function of a mediator-accelerator of decay for them, is noted. The possibilities of practical application of shungite for the effective use of therapeutic natural waters of the Altai are evaluated. The effect of structuring water systems after contact with shungite has been established, based on changes in three main physico-chemical parameters: redox potential, specific electrical conductivity, and pH. The paper presents possible options and mechanisms for structuring water systems based on mineral therapeutic radon waters of Altai in their contact with shungite due to the presence of molecular carbon-fullerene in it. Based on the peculiarities of the RP change, new scientific data on the various effects of interaction of Altai radon therapeutic waters with fullerenes have been established. The possibility of both increasing and decreasing the redox potential has been experimentally proven, which makes it possible, if necessary, to radically change the therapeutic properties and functions of mineral radon waters.

Shubhangi R. Sonawane   and Sanjay B. Patil   

Nitrendipine is used in the treatment of hypertension. It comes under BCS class II and has a poor dissolution rate and water solubility. In the present study, pharmaceutical cocrystals of nitrendipine with 4-hydroxy benzoic acid were prepared using crystal engineering, an innovative method for improving solubility. 4-hydroxy benzoic acid was used as a co-former to prepare cocrystals of nitrendipine in the ratios of 1:1 and 1:2. Nitrendipine cocrystals were prepared using cooling co-crystallization. The prepared cocrystals were assessed for in vitro dissolution characteristics, saturation solubility, and stability. Analytical measures such as Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC) were also used to analyze cocrystals for their purity and to confirm the formation of cocrystals. By using the cooling co-crystallization process, nitrendipine and 4-hydroxy benzoic acid crystallize together in an equimolar ratio. When compared to pure nitrendipine, the nitrendipine - 4-hydroxy benzoic acid cocrystals have a dissolving rate that is 3-4 times faster. Co-crystallization may increase nitrendipine's water solubility and rate of dissolution, which could be a solution to the drug's bioavailability issue. X-ray diffraction revealed crucial hydrogen bonding and interactions, while differential scanning calorimetry confirmed improved dissolution kinetics and higher equilibrium solubility in the optimized nitrendipine cocrystal formulation. Nitrendipine's solubility and dissolution rate are improved by the cocrystal formulation, according to the results of research on its solubility, dissolution, and stability.

Deepak Jha   and Ashish Singh Parihar   

The current study evaluates the toxicological safety and antioxidant potential of an ethanolic extract mixture from Ziziphus mauritiana and Bauhinia racemosa leaves, two plants with significant ethnopharmacological and therapeutic value. Acute oral toxicity was evaluated in Wistar rats following the guidelines outlined by the Organization for Economic Co-operation and Development (OECD) 423 protocol, with the extract mixture administered in doses reaching 2000 mg/kg of body weight. No adverse effects or mortality were observed over a 14-day period, indicating a high margin of safety. Antioxidant activity was evaluated by measuring total phenolic content (TPC), and total flavonoid content (TFC) and through the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. The extract exhibited substantial phenolic (7.75 mg GAE/g) and flavonoid (6.70 mg QE/g) contents, both associated with strong antioxidant properties. The DPPH assay revealed an IC₅₀ value of 75.53 ÎĽg/mL, demonstrating notable antioxidant activity, though less potent than synthetic antioxidants like ascorbic acid (IC₅₀ = 24.96 ÎĽg/mL). The result indicates that the ethanolic extract mixture of Z. mauritiana and B. racemosa leaves is safe for pharmacological use, supporting their traditional application with minimal toxicity risk at standard doses. However, chronic toxicity studies are recommended to establish long-term safety. This research lays the groundwork for the development of natural antioxidant therapies, highlighting the therapeutic potential of the Z. mauritiana and B. racemosa extract mixture in combating oxidative stress-related diseases.

Priya Dipak Jagtap   Reshma Vijay Jadhav   Ashish Suresh Jain   Bhavesh Dilip Mahajan   Prapti Jagdish Gawand   and Prathamesh Vitthal Chaudhari   

The orodispersible liquisolid system represents an innovative breakthrough in the pharmaceutical field. It combines liquisolid technology with the orodispersible system. In recent years, many drug candidates have been formulated, most of which are lipophilic with poor water solubility. The liquisolid system is ideal for such drugs that exhibit low or no water solubility, possess high permeability (BCS Class II), and necessitate either sustained or immediate release. Powder solution technology, also known as liquisolid formulation, is the process of transforming liquid pharmaceuticals (drugs in solution or suspension) in non-volatile solvents by mixing the solution with suitable carriers and coating agents to create cohesive-free, readily flowable, and compressible powder blends. Orodispersible tablets are becoming more popular as innovative oral drug delivery systems because they can break down into smaller granules or a gel-like form in less than three minutes, making it easier for patients to swallow. Orodispersible tablets provide a fast onset of action due to the inclusion of super disintegrants, which allows for quick absorption through the medication's pre-gastric uptake from the palate, throat, and oesophagus during the swallowing of saliva. This aids in dose reduction. Furthermore, they promote patient compliance and enable proper oral administration for children and elderly individuals who find it challenging to swallow. By using both liquisolid and orodispersible systems, one may improve the dissolution speed, solubility, and bioavailability of medications while achieving a rapid onset of accompanying pharmacodynamic effects. This review study significantly helps readers and researchers understand this novel pharmaceutical dosage form. This article explores the concept and practical use of the orodispersible liquisolid compact method to enhance bioavailability and solubility.

Anjali Rajan   and Bindhu K. B.   

Seaweeds are an abundant reservoir of bioactive compounds with prospective utilization in multidisciplinary domains, particularly in pharmacology. Algal samples were collected from the Southeastern coast of India. Extracts were prepared using water and ethanol as solvents. BSLA can be considered a propitious preliminary toxicity test, as the brine shrimp is acutely responsive to a variety of chemical substances. Trypan blue exclusion method can be described as a straightforward and cost-conscious method for the preliminary cytotoxic examination of natural extracts, using DLA cells and normal spleen cells, in which the degree of cytotoxicity is evaluated concerning the percentage of mortality of cell lines. A dose-dependent increase in the percentage of dead cells demonstrates cytotoxic competence of the extract. Conversely, a higher percentile of live cells reveals the selective cytotoxicity of the extract against cancer cells, which is a favorable attribute of anticancer drugs. The aqueous and ethanolic extracts of Stoechospermum marginatum, with an LC₅₀ value of 460 and 420 µl/mL, respectively, had the highest cytotoxicity on the brine shrimp larvae compared to aqueous and ethanolic extracts of Sargassum wightii. Strikingly, the ethanolic extracts of both algae demonstrated the highest cytotoxic capability against DLA cells, with LC₅₀ values of 30.61 and 10.75 µl/mL, while exhibiting comparatively low toxicity towards normal spleen cells. These inferences signify that the ethanolic extracts of Sargassum wightii and Stoechospermum marginatum possess bioactive compounds with promised anticancer properties and minimal toxicity against normal spleen cells, justifying intensified inspection for the isolation and characterization of the active constituents responsible for the remarked cytotoxic effects.

Nischith Sirawase Shankar   Maged Alkanad   VidyaShree Nagamangala SundarRaj   Yogesh Kumar Shivakumar   Ghada Alhamdani   Amutanand Tripathy Sachidanand   and Annegowda Hardur Venkatappa   

Both conventional and modern medicine rely on traditional herbs due to their medicinal effectiveness and low side effects. Some of these, like Annona species, are used as food because their fruits are edible, and scientists have shown that they contain many bioactive substances, such as alkaloids, peptides, lectins, acetogenins, isoquinalones, and volatile oils. These molecules emphasize their pharmacological relevance and help explain the therapeutic actions of plants. The goal of this review is to look at the medicinal potential of Annona species, especially Annona squamosa, A. reticulata, and A. muricata. These species have a lot of useful medical properties, such as the ability to fight diabetes, bacteria, cancer, fungi, blood vessel growth, seizures, inflammation, and blood vessel relaxation. This review combines the traditional use, phytochemical composition, and therapeutic qualities of these species using current information. Methodologies used in this review comprise a thorough analysis of scientific studies concerning the Annona species and present literature. Among other health advantages, the main findings show that the bioactive chemicals in these plants can help collagen and elastin synthesis, lower oxidative stress, and increase skin moisture. The main findings of this research highlight the great therapeutic value of Annona species, offering natural solutions for the management and treatment of many diseases. By stressing the two advantages of these plants that they satisfy demand for more efficient treatments and help to solve the growing issue of drug resistance this work improves the field. Moreover, it highlights the important part Annona species play in both conventional and modern medicine, therefore opening the path for the creation of fresh plant-based medicinal agents.

Shrutika Kambhale   and Jyotsna Chopade   

Mass spectrometry (MS), which provides unparalleled sensitivity, precision, and versatility for identifying and characterizing complex chemical compounds, has transformed metabolite profiling in medicinal plant research. This paper examines how MS can be used to profile primary and secondary metabolites that are essential to the pharmacological characteristics of medicinal plants, such as sugars, amino acids, alkaloids, flavonoids, terpenoids, and phenolics. Even in complex plant matrices, MS techniques like high-resolution mass spectrometry (HRMS) and tandem mass spectrometry (MS/MS) offer detailed structural elucidation of bioactive compounds. Our capacity to understand the metabolic complexity of medicinal plants has been greatly improved by the combination of targeted and untargeted metabolomics techniques. While untargeted metabolomics makes it easier to find new chemicals and identify metabolic pathways, targeted metabolomics concentrates on quantifying existing metabolites with particular therapeutic value. The resolution and dependability of metabolite detection are further improved by the application of sophisticated separation techniques, such as gas chromatography-mass spectrometry (GC-MS) and liquid chromatography-mass spectrometry (LC-MS). Through standardization and authentication procedures, MS contributes significantly to the quality, safety, and effectiveness of medicinal plant products beyond metabolite identification. MS-based metabolomics helps the creation of evidence-based plant-derived medications and verifies traditional medicinal claims by bridging the gap between traditional knowledge and contemporary analytical research. Additionally, MS applications support the sustainable use of plant resources by extending to ecological and conservation studies. The developments, difficulties, and potential paths in MS-based metabolomics for medicinal plants are highlighted in this study. It highlights how MS can be a key component of medication development and discovery, with a focus on phytochemical research, the identification of bioactive compounds, and therapeutic standardization. Researchers can increase the scientific basis of traditional medicine and promote innovation in the creation of plant-based therapies by utilizing MS technology to open up new avenues for natural product research.

J. Josephine Leno Jenita   Pasupathy A   Seema S. Rathore   and Wilson Barnabas   

Currently, nanotechnology-mediated drug delivery systems are targeted towards cancer therapy. The guar gum and ethyl cellulose nanoparticle-based delivery system developed in this study demonstrates the potential of nanotechnology-mediated approaches for the targeted and sustained delivery of capecitabine in managing colorectal cancer. Guar gum and Ethyl cellulose have been selected as polymers to formulate NPs for colon targeting. Different batches of drug-loaded GG-EC NPs were prepared by the emulsion solvent diffusion method. The optimal batch exhibited a particle dimension of 235.6 ± 4.28 nm with a polydispersity index (PDI) of 0.153 and a zeta potential of -23.4 ± 3.12 millivolts. The in vitro drug release pattern demonstrated that the liberation of capecitabine was sustained for 24 hours. The mechanism of drug release from formulated NPs was followed with Non-Fickian mediated with diffusion-controlled. Animal studies determined the targeting efficiency of the ideal formulation. Results indicated that the concentration of capecitabine was higher than the standard drug. The distinctive characteristics of the polymers employed in the nanoparticle formulation facilitate specific drug discharge in the colon, diminishing systemic contact and amplifying remedial effectiveness.

Ismail Gamal Ismail Ali   Amal W. Danial   Ahmed Shawky Mohamed Mousa   and Maged Sayed Ahmed   

The rise of multidrug-resistant (MDR) infections poses a significant threat to global health, challenging the efficacy of existing antibiotics and leading to increased morbidity and mortality. This alarming trend necessitates an urgent search for novel bioactive substances from environmental sources, particularly soil microorganisms, which have historically been a rich reservoir of antibiotics. Streptomyces, a genus of Gram-positive bacteria found predominantly in soil, has been a prolific source of antibiotics, contributing significantly to the arsenal of antimicrobial agents available today. Nine soil Actinomycetes were isolated from soil samples, purified, and then screened in the current investigation to determine the antibacterial potential of new Actinomycetes. Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and other multidrug-resistant bacteria were the focus of both primary and secondary screening. The most active isolate, identified as Streptomyces werraensis, was selected for further investigation. Microbial strain was determined based on morphological, biochemical, and genetic characteristics. From our study, thirteen antibacterial substances were identified, and the most active compound was phenol, 2,4-bis (1,1-dimethylethyl), which demonstrated potent antibacterial properties against a range of MDR bacteria. Advanced analytical techniques, such as mass spectrometry are used to identify the bioactive compounds. This research addresses a critical need in the fight against MDR infections by exploring untapped environmental sources for new antibiotics. The findings could lead to the development of novel therapeutic agents, thereby contributing to global health and the management of antibiotic resistance.

Ibrahim Konneh   Cenk Serhan Ozverel   Emine Erdag   and Nazife Sultanoglu   

Sexually transmitted diseases (STDs) caused by viruses such as HIV and HCV remain a global health concern. Antiviral resistance is increasing due to viral mutations, necessitating the search for novel therapeutic candidates. This study evaluated the binding affinities and potential efficacy of eleven antiviral drugs and a drug candidate, AVG-388, using in silico methods against HIV and HCV target proteins. Molecular docking simulations were performed using AutoDock Vina, followed by MM/PBSA calculations to determine binding free energies. Molecular dynamics simulations were conducted using GROMACS, and Monte Carlo simulations modeled the variability in binding energies. A 3D energy landscape was mapped using Matplotlib, and a multivariate regression analysis was conducted to correlate binding energies with predicted ligand efficacy. As a result, AVG-388 demonstrated consistently strong binding affinities across HIV and HCV targets. The binding energy for HIV reverse transcriptase was -171.15 ± 2.42 kJ/mol and for HCV RdRp NS5B was -226.21 ± 3.25 kJ/mol. Sofosbuvir showed stronger binding for HCV (-256.26 ± 2.36 kJ/mol) but was less effective against HIV. Statistical analysis revealed that AVG-388 outperformed several FDA-approved antivirals, such as Remdesivir and Molnupiravir, in dual-target inhibition potential. The study highlights AVG-388 as a promising broad-spectrum antiviral candidate, demonstrating superior binding affinities for both HIV and HCV. Further in vitro and clinical evaluations are necessary to confirm its potential for treating STDs and overcoming resistance to viral infections.

Samten Doma Sherpa   Tiewlasubon Uriah Khar   and Sonam Bhutia   

The present survey was conducted in Sikkim's south and east districts and interacted with 6 traditional healers/informants from the selected areas. The methodology adopted during the survey was face-to-face interview, field survey, open-ended survey, and pre-prepared semi-structured questionnaires. A total of 30 ethnomedicinal plant species belonging to 24 families, 25 genera were presented in this work for the treatment of jaundice by the traditional healers from Gangtok and Namchi districts of Sikkim. The study revealed that the most of the traditional healers were more the 50 years of age, 6/6 (100%) were male and are mainly herbalist; all were literate, done middle level of education at least (50%). Based on plant family utilization, Asreraceae and Rutaceae (10%) followed by Fabaceae, Aristolochiaceae and Berberidaceae (5%) were reported. Further, root followed by leaf and stem are the highest plant parts used and the most commonly used form of preparation was juice followed by decoction. In case of mode of administration, oral route of administration was highest as compare to topical route. The ethno-botanical index-Use Value (UV)-0.83 was found to be highest for Cuscuta reflexa followed by Curcuma longa (0.5), Andrographics paniculate (0.5) respectively. From the findings, it was revealed that, the traditional healers are using the different plants to treat jaundice since ages with different types of preparations. Therefore, such traditional knowledge should be explored more for the scientific development and motivate such practices leading edge in pharmacological activity found in these plants having more UV value may lead to the identification of novel therapeutic candidates in the future.

Sowmya KM   and Narendhirakannan RT   

This study investigates the phytochemical composition, antimicrobial, antioxidant, and anticancer activities of the aqueous, chloroform, and ethanol extracts of Elettaria cardamomum pods. Phytochemical screening revealed the presence of alkaloids and flavonoids in the aqueous extract, cardiac glycosides and alkaloids in the ethanol extract, and only cardiac glycosides in the chloroform extract, with tannins, terpenoids, and saponins absent across all extracts. Focusing on flavonoids, the total flavonoid content of the aqueous extract was quantified at 45.5 ± 0.12 µg/mL using the aluminum chloride method. Antimicrobial assays demonstrated that the aqueous extract inhibited both Gram-positive and Gram-negative bacteria, with the highest inhibitory effect observed against Pseudomonas aeruginosa (18±0.02 mm zone of inhibition at 100 µg/mL). The extract also exhibited significant antioxidant properties, displaying effective DPPH scavenging (IC₅₀ = 20.44 ± 0.23 µg/mL), ABTS radical inhibition (IC₅₀ = 10.324±0.23 µg/mL), and nitric oxide scavenging (IC₅₀ = 21.78±0.18 µg/mL). Additionally, the anticancer potential was assessed via MTT assay, showing significant growth inhibition of the HT-29 colorectal cancer cell line (IC₅₀ = 67.98 µg/mL), with maximum inhibition at 300 µg/mL (71.93%). The findings of this study highlight the therapeutic potential of E. cardamomum pods as a source of bioactive compounds with notable antimicrobial, antioxidant, and anticancer activities. These results support further exploration of E. cardamomum in medicinal applications, emphasizing its role as a valuable natural product in combating oxidative stress and cancer. Future research should aim to isolate and characterize the specific compounds responsible for these bioactivities to develop effective therapeutic agents.

Yogesh B. Gajmal   Padma L. Ladda   Nilofar S. Naikwade   and Salma Bagwan   

Chemotherapy-induced immunosuppression is a common side effect of chemotherapeutic agents like 5-Fluorouracil (5-FU), which can compromise the body's immune defense and increase susceptibility to infections. The present study aimed to evaluate the potential of Terminalia bellirica fruit extract (TBFE) and Adhatoda vasica Linn. leaf extract (AVLE) in alleviating the immunosuppressive effects induced by 5-FU in Wistar albino rats. Phytochemical screening of TBFE and AVLE revealed the presence of bioactive compounds, including flavonoids, proteins, amino acids, glycosides, alkaloids, phenolic compounds, and tannins, which are likely responsible for their immunomodulatory effects. To assess the immunostimulatory activity, various in-vivo and ex-vivo methods were employed, including delayed hypersensitivity reaction, carbon clearance test, neutrophil adhesion test, and T-cell population analysis. The results demonstrated that both TBFE and AVLE significantly (PË‚0.05) ameliorated the 5-FU-induced immunosuppression. Treatment with the extracts enhanced paw edema following antigen challenge, increased neutrophil counts, phagocytic activity, total lymphocyte count, and rossette formation. These findings suggest that the ethanolic extracts of TBFE and AVLE have the potential to restore immune function in 5-FU-treated rats, highlighting their potential as natural immunostimulants in chemotherapy-associated immunosuppression. Although promising, further studies are needed to explore the molecular mechanisms underlying their effects and to establish optimal dosages for clinical applications. This study contributes to the growing body of research on plant-based immunomodulators, with implications for improving the quality of life in cancer patients undergoing chemotherapy.

Avinash A. Gunjal   Ashish V. Kulkarni   Devendra S. Shirode   Prasad K. Bairagi   Vasant Y. Chavan   and Niraj S. Vyawahare   

Background and Objectives: L-carnitine (LC), a critical component in producing cellular energy and the catabolism of fatty acids across various species including mammals, plants, and specific bacteria, is recognized for its anti-inflammatory and antioxidant activities. The primary goal of this investigation was to examine the potential of L-carnitine-L-tartrate (LCLT) as a supplement in treating hemorrhoids by using the Jatropha oil-induced hemorrhoid model. Materials and Methods: LCLT was sourced from Sigma Aldrich, USA. Hemorrhoids were experimentally induced in the anorectal regions of rats by applying Jatropha oil. The rats were subsequently administered LCLT (300 mg/kg, p.o and 500 mg/kg, p.o) along with Pilex granules (400 mg/kg, p.o) as a reference treatment, for 10 days. On the final day of treatment, anti-hemorrhoidal efficacy was assessed by measuring body weight, severity score, rectoanal coefficient (RAC), and conducting histopathological analysis of anorectal tissue. Results: LCLT supplementation resulted in a significant increase in body weight, decreased severity scores, and reduced rectoanal coefficient. Histopathological analysis further revealed a substantial decrease in inflammatory responses. Conclusion: The findings suggest that LCLT, likely through the action of carnitine, exhibits significant anti-inflammatory and antioxidant effects, making it a promising supplementary treatment for hemorrhoids.

Chinelo Anthonia Ezeabara   Adaobi Maureen Obi-Nwoye   Ebubechukwu Princewill Okoye   and Wisdom Chibuzo Anyanele   

Costus afer Ker Gawl. is an erect, evergreen herbaceous plant with spirally arranged leaves, belonging to the family Costaceae. This study aimed to investigate the morphological, anatomical, phytochemical characters, and antimicrobial activity of the plant. Anatomical studies were carried out using paraffin wax embedding technique while morphological studies and phytochemical analysis were conducted using standard laboratory methods. The antimicrobial activity was evaluated using in vitro assays, including agar well diffusion and broth microdilution methods. Significant differences were determined using Duncan's Multiple Range Test (DMRT). The results revealed distinctive morphological and anatomical features, including entire leaf margins, collateral and closed vascular bundles, and a light hair-like structure around the stem. Phytochemical analysis detected the presence of alkaloids, flavonoids, phenols, saponins, steroids, tannins, and terpenoids in the leaf, stem, and root. The plant's extracts demonstrated a dose-dependent inhibitory effect against the tested bacterial and fungal pathogens, indicating a potential therapeutic application. Aspergillus fumigatus was the most susceptible to the plant extracts. The blend of root and stem extract showed strong antibacterial activity against Heampophilus infleunzae, Salmonella typhi, Streptococcus agalactiae, and Vibro cholera. The findings provide valuable information on the botanical and phytochemical properties of C. afer, highlighting its potential as a source of antimicrobial agents.

Shilpaja Chella   and Saravanakumar Kasimedu   

The creation of an in-situ nasal gel of Metoclopramide Hydrochloride represents a promising innovation in drug delivery technology, providing an effective and patient-friendly alternative to conventional oral formulations. The prolonged release and higher absorption attained by this formulation may result in better treatment outcomes for patients suffering from chemotherapy-induced nausea and migraines. All formulations were thoroughly tested for physicochemical parameters such as pH, viscosity, mucoadhesive strength and drug content to ensure they satisfied the requirements for nasal delivery. In-vitro dissolution studies were performed to examine the gel's drug release profile and the results revealed that the gel has sustained release characteristics, which are critical for sustaining therapeutic drug concentrations over time. Increasing the concentration of mucoadhesive polymers (Poloxamer 407 and Carbopol 934) enhanced viscosity and mucoadhesive strength, resulting in a more controlled release of Metoclopramide Hydrochloride from the formulation. Poloxamer 407, a mucoadhesive polymer, Carbopol 934, a sensitive to pH polymer and PEG 400, a permeation enhancer were all incorporated in the formulation. In-vitro dissolving studies were used to characterize the release profile of Metoclopramide Hydrochloride from nasal gel formulations. The results showed that increasing the concentration of the mucoadhesive and pH-sensitive polymers (Poloxamer 407 and Carbopol 934) resulted in an increase in gel viscosity and mucoadhesive strength. This increase in viscosity helped to produce a more robust gel network, slowing the drug's diffusion and resulting in a more regulated and prolonged release over time. The optimal formulation, with carefully balanced polymer concentrations, demonstrated effective sol-gel conversion, sustained drug release, and improved bioavailability.

Prapti J Gawand   Reshma Jadhav   Ashish S Jain   Priya J Jagtap   Bhavesh D Mahajan   and Prathamesh V Chaudhari   

An autosomal recessive genetic condition with a high frequency in populations of European descent is hemochromatosis. Reports indicate that 60% to 90% individuals of European descent exhibit a mutation linked to hemochromatosis. A hereditary or acquired illness called hemochromatosis is brought on by an individual's body storing too much iron. The pathogenetic approach of chronic, excessive dietary iron absorption coupled with the breakdown of normal regulatory systems contributes to hemochromatosis. As a result, ferritin, especially hemosiderin, which is a kind of stored iron, gradually but significantly rises. The human body needs iron to function normally on a daily basis and to be healthy. On the other hand, too much iron caused the hazardous circumstances. Hemochromatosis can lead to an iron buildup that affects many bodily systems and organs, including the heart, liver, pancreas, endocrine glands, and joints. In healthy individuals, feedback systems impede the absorption of iron as stored iron levels rise. Dietary restrictions, such as consuming green tea, are required to reduce the absorption of iron. A great plant supplement for healthy liver function is turmeric. Diseases brought on by an excess of iron can be successfully treated with a variety of herbal supplements. Plant-based vitamins such as manjishta, spirulina, and neem aid in the efficient treatment of hemochromatosis. Chinese herbal remedies are also incredibly powerful. When iron overload occurs, scavenging surplus iron can be beneficial. During this period, iron overload can be controlled with the use of botanical chelators. Antioxidant and iron chelation activities work well. Supplemental nutrition also aids in controlling iron excess symptoms. Maintaining an individual's body's iron load is another benefit of taking dietary supplements.

Shreya Jadyal   and Pallavi M. Chaudhari   

Depression is one of the serious and common mental health problems. In a depressed state, one feels low, feeble, helpless, which ultimately affects the physical health, thoughts and normal functioning of life like (eating, sleeping). Oral administration is one of the non-invasive methods widely used to introduce antidepressants, which has high patient compliance as compared to invasive methods such as intracerebral, intrathecal, intracerebroventricular. But antidepressants include neuropeptides, natural active ingredients, and certain chemical agents whose bioavailability is restricted due to BBB and first-pass metabolism. To prevail over these challenges and enhance drug availability in the brain, researchers are exploring alternative delivery methods and novel formulations. The intranasal route is one such alternative that bypasses the BBB. Additionally, innovative formulations like solid lipid nanoparticles, gold nanoparticles, polymeric nanoparticles, dendrimers, nano emulsion, liposomes, niosomes, nanostructured lipid carrier, are being developed to enhance drug delivery to the brain. SLNs are particularly promising. These sub-micron colloidal carriers, composed of lipids dispersed in water, offer higher entrapment efficiency compared to niosomes and liposomes. By utilizing these modern drug delivery approaches, researchers aim to improve the efficacy of depression therapy by ensuring that a significant fraction of the delivered drug reaches its target by crossing the BBB.

Shirode Devendra   Patil Aishwarya   Gauri Gawande   Agrawal Amit   and Bindurani LGP Ram   

Type 1 Diabetes is non-communicable chronic metabolic disease and the causes are due to autoimmunity destruction of beta cells of pancreas occurs along with dyslipidaemia. Type 1 diabetes become the main cause of mortality. Insulin is the only therapy still available for treatment of type 1 diabetes but has side effects. There is need to develop such a formulation which has base of herbal medicines. The current work's goal is to develop a polyherbal formulation (Hugonia Mystax: Blumea Lacera: 1:1) and investigate it against hyperglycaemia. Single dose of freshly prepared alloxan monohydrate (120mg/kg) was given to animals to introduce diabetes in rats. After 48 hours the animals were selected for treatment of polyherbal formulation for next 14 days. At the end of the study, evaluation of body weight, blood glucose level, lipid profile, glycosylated haemoglobin level and histopathological pancreas of rat were done. The result elaborated that polyherbal formulation showed significant reduction or normalization of parameters which were altered by induced alloxan. The results estimated support that polyherbal formulation has potential livelihood towards various anti-diabetic mechanisms specially on healing of damaged beta cells. The result of present study revealed polyherbal formulation has anti hyper glycaemic effect and anti-hyperlipidaemic activity by regulating blood glucose levels and lipid profile.

Hitarthi Patel   Meenakshi Patel   and Lalit Lata Jha   

When it comes to pharmacotherapy, children and adults have different abilities towards drug administration and taste acceptability. Pediatric medications must be designed to best meet the age of a child, physiologic condition, size, and therapeutic needs. The existing dosage forms available have various drawbacks, which result in poor pediatric patient compliance. This review explores the significance of pellet-based formulations in pediatric drug delivery, emphasizing the extrusion-spheronization technique as a versatile and effective method for developing multiparticulate oral dosage forms. Pellets produced through this method exhibit uniformity in size and shape, improved drug stability, controlled release profiles, and the potential for taste masking—features critical for ensuring accurate dosing and enhanced patient compliance in children. Furthermore, it provides an in-depth discussion of the fundamental principles of pellet development, detailing key stages such as nucleation, coalescence, layering, and abrasion. It also covers various pelletization techniques, with a special focus on extrusion-spheronization, highlighting its advantages over other methods. Factors influencing pellet quality, including formulation components (e.g., excipients, moisture content, granulating fluids) and process parameters (e.g., equipment type, extrusion speed, spheronization conditions), are thoroughly examined. Recent research studies and marketed products using extrusion-spheronization for pediatric applications are reviewed to exhibit the practical potential and clinical significance of this technology. These include taste-masked, fast-disintegrating, and dual-release pellet formulations designed to satisfy the specific needs of pediatric patients. The review concludes that extrusion-spheronization is a promising platform for developing innovative pediatric dosage forms that improve therapeutic outcomes and patient experience. By addressing existing limitations in pediatric drug delivery, this approach contributes to safer, more effective, and more acceptable treatments for children.

Riya K. Mehta   Yash D. Dudhwala   Nandini M. Gamit   Vipul G. Gajera   and Ketan V. Shah   

Clinical trials for novel pharmaceuticals are expensive in terms of both financial costs and human health when unexpected human safety problems occur. Through preclinical safety testing, the drug development industry tries to reduce these occurrences. Many medical studies use animal models to learn more about the causes of animal and human diseases, as well as to develop new treatment measure. The zebrafish (Danio rerio) exhibits a variety of traits that make it a useful model for research on human genetics and illness. The zebrafish is a useful experimental model for behavioural, genetic, and toxicological research that elucidates the mechanisms behind a variety of human disorders. It is also useful for evaluating new treatment agents, such as the safety of new vaccines. The zebrafish model is a bridge between in vitro assays and mammalian in vivo studies. In the last few years, the use of zebrafish (Danio rerio) as well-established animal model system for nanoparticle toxicity assessment has expanded dramatically. The zebrafish holds the chance of making contributions to a number of tiers of the drug improvement process, such as target identity, disease modelling, lead finding, and toxicity. This review summarizes that Zebra fish have been used as potential experimental models in a number of research.

Vidhan Chand Bala   Bhawna Diwakar   Arvind Kumar Patel   and Sushil Kumar   

The recent trend worldwide is searching for plant extracts to prevent neurodegenerative disorders. The aim of this study is to conduct the phytochemical screening to explore neuroprotective effects of Madhuca indica leaf ethanol extract (MLE) in rats. Chemical composition was screened by using phytochemical screening tests and HPTLC methods. The neuroprotective effect was analyzed by Immobilized stress tolerance test, Elevated plus maze test, and Morris water maze test. The result of this study reflected that ethanolic extract from Madhuca Indica leaves was valuable in all methods in the dose-dependence approach. The findings show that, in comparison to the amnesia control group, the MLE significantly lowered the levels of metabolic markers like glucose, cholesterol, urea, and nitrogen increased escape latency (EL), and lowered the transfer latency (TL). Based on the aforementioned useful animal study, we have determined that MLE considerably affects neuroprotective activity compared to the amnesia control group. We may therefore conclude that Madhuca indica is highly successful in all test models and that it may be utilized to treat CNS illnesses by enhancing their effects and minimizing their negative effects in combination with currently marketed medications.

Akshay K Patil   Adarsh C Umarani   Sushant Madar   Srushti Murgod   and Simran Gawas   

The objective of current research work was to develop quality by design based simple stability indicating UV Spectrophotometric method for simultaneous analysis of trigonelline and piperine and its application to prepared nanoformulation. A simple, cost economic method was developed and validated as per ICH guidelines. Design of experiment was used to optimize the method where sonication time and scanning interval were identified as independent variables and absorbance was considered as a dependent variable. A simple 3² full factorial design with 9 runs was used to optimize the method. Water is used as a major solvent. The optimized run (10 min sonication time and medium scanning interval) was extensively validated as per ICH guidelines. A forced degradation study was also carried out. Furthermore, the devised method was successfully applied for the estimation of drugs in prepared nanoformulation. Based on the result, the method was found to be simple, accurate, precise, and robust as evidenced by validation parameters which all fall within acceptance limits. A linear relationship was determined between the concentration ranging from 2 to 10 /ml, with a regression coefficient of 0.999 for trigonelline (265nm) and piperine (342nm). Both precision assays showed a percent RSD of less than 2 indicating the precise nature of the method. The percentage recovery ranged from 99.54 to 101.43 % for trigonelline and 99.88 to 101.83 % for piperine, indicating promising accuracy. Trigonelline showed LOD and LOQ values of 1.064 /mL and 3.22 /mL and piperine showed 0.814 /mL and 2.46 /mL respectively which proves the sensitive nature of the method. Percent RSD less than 2 indicates that the developed method is rugged and robust. Further, acidic, basic and oxidative degradation was in the range of 10- 19% whereas photolytic assay showed pronounced degradation characteristics (44-52%). Additionally, the developed method was successfully utilized for the estimation of trigonelline and piperine in prepared nanoformulations. Therefore, it can be inferred that the current study will serve as a foundation for the quality assessment of trigonelline and piperine naanoformulation utilizing the Quality by Design approach.

Raghavendra Kumar Gunda   A. Vijayalakshmi   Prathap Madeswara Guptha   Koteswara Rao GSN   Kondapuram Parameshwar   and Madhavi Latha Chennuru   

Objective: The purpose of the present research work was to develop Sulforaphane loaded magnetic nanoparticles (MNPs) and the effect of prepared magnetic nanoparticle on the enhancement of bioavailability, stability, and dissolution was studied. Sulforaphane (SFP) is a naturally occurring isothiocyanate and chiefly available in broccoli. Methods: Magnetic Nanoparticles were prepared by encapsulating herbal drug SFP with iron salts and the prepared magnetic nanoparticles were analyzed by Infrared Spectroscopy, Crystal Analysis, Scanning Electron Microscope (SEM), Thermal Analysis, Drug Loading Efficiency, Magnetic Analysis, Electrical Analysis and Stability Studies. Results: The obtained data of the characterization studies reveal that the magnetic nanoparticles (MNPs) have good holding properties. The particles sizes of MNPs measured from High Resolution Scanning Electron Microscopy (HRSEM) were of ideal size range 100 - 250 nm and showed a regular pattern of spherical shape. The Vibrating Sample Magnetism (VSM) results showed satisfactory value. The pH of the medium has an inverse relationship with the amount of Sulphoraphane released by the MNPs. Conclusion: From the results, the current study concludes that the prepared MNPs (four types) are structurally arranged following a good pattern, sufficient amount of elements with good size range over the particle surface, and exhibit magnetic responsiveness which is sufficient for drug target due to an external magnetic field because of its pore volume and large surface area. Dissolution study reveals that the prepared Sulforaphane loaded MNPs of Iron-MCM-41 showed maximum drug release at pH 5.5.

Mitali Kubade   Priya Shetti   and Ramesh Paranjape   

Background: Chromolaena odorata (Siam weed) is a perennial shrub used in the treatment of many ailments and disease conditions, also known as Siam weed. A potential weed of tropical and sub-tropical regions inhabits waterways. The medicinal values of Chromolaena odorata lie in their phytochemical's component. The present study aims to develop and validate an UV spectrophotometric method according to ICH guidelines for the estimation of C. odorata. Materials and Method: The study is focused on generating a specific, linear, accurate and precise UV spectrophotometric method for estimation of aqueous C. odorata. The method's parameters were assessed within a concentration range of 0.2 µg/ml - 1 µg/ml, with recovery rates specifying accuracy and low % relative standard deviation (RSD) values confirming precision. Limits of detection (LOD) and quantification (LOQ) for C. odorata were determined. Results and Discussion: Validation is conducted to ensure that the analytical methods are accurate, specific, reproducible, and resistant to the analyte range to be analyzed. The method was validated for many parameters. Solvent development step involves the use of water in which Siam showed spectrum with maximum absorbance at 211nm. A coefficient of correlation of 0.9975 was discovered in accordance with Beer's law. After determining the technique's sensitivity, the limit of detection and limit of quantification were determined to be 1.07 µg/ml and 3.25 µg/ml, respectively. Conclusion: In conclusion, the development and validation of a UV-visible spectrophotometric method for the estimation of aqueous Chromolaena odorata extracts demonstrate a promising approach for routine quality control analysis. The method offers a simple, cost-effective, and efficient means of analysis when adequately optimized. The validation according to ICH Q2 (R1) guidelines confirms that the method meets the necessary acceptance criteria, making it suitable for the routine analysis of Chromolaena odorata.

Pallavi Kaushik   Ram Niwas Jangir   Vinod Kumari   Neetu Kachhwaha   Geeta Meena   Shashi Meena   Ruchi Vyas   Aditya Jain   Anu Yadav   Nitesh Gupta   and P. C. Mali   

The contemporary area of antimicrobial research is witnessing a transformation with the advent of novel strategies, prominently exemplified by antimicrobial nanoparticles. This review explores this emerging field of antimicrobial nanoparticles, focusing on the efficacy of silver nanoparticles (AgNPs) as powerful means against microbial threats. Addressing the pressing concern of antibiotic resistance, the article underscores the importance of novel approaches. A key highlight is the environment-friendly production of AgNPs derived from various microbial and plant origins, providing sustainable synthesis approaches. The review thoroughly explains how AgNPs combat microbes, utilizing mechanisms such as reactive oxygen species generation and subtle alterations in cellular functions. Beyond theoretical discussions, the practical applications of AgNPs are explored through the study of clinical researches, showcasing their potential in real-world scenarios. By combining insights from these studies, the review underscores AgNPs as promising candidates for effective antimicrobial interventions. It amalgamates eco-friendly synthesis, mechanisms of action, and clinical trial perspectives, positioning AgNPs as valuable players in the ongoing battle against microbial threats. The overview provided here, not only enhances our understanding of AgNPs' antimicrobial capabilities but also points towards future research and development directions. Overall, the review contributes to emphasizing the shift towards innovative, environmentally conscious solutions in the face of escalating microbial challenges.

Garima Kapoor   Rubina Bhutani   Navidha Aggarwal   Kandasamy Nagarajan   and Pooja Gangwar   

Catharanthus roseus (L.), also known as Madagascar periwinkle or Sadabahar, is a significant Apocynaceae family plant renowned for its medicinal properties. Catharanthus is having many beneficial alkaloids for treating diabetes, stomach issues, high blood pressure, asthma, menstrual problems, and cancer. The plant has two main cultivars, "Rosea" with pink flowers and "Alba" with white flowers. Various parts of the plant have been used traditionally in different cultures. In Brazil, an infusion of leaves is used as a mouthwash for tooth pain, to treat hemorrhage and scurvy, and to heal chronic wounds. In the West Indies and the Philippines, it is used for diabetes-related ulcers and as an oral anti-diabetic drug. The plant is also known for its antibacterial and hypotensive effects, although the latter has not been fully substantiated. The most potent components of C. roseus are its alkaloids, with over 400 identified. These alkaloids are utilized in insecticides, fragrances, food additives, medicines, and agrochemicals. The plant's roots and stems contain alkaloids like ajmalicine, vinblastine, and vincristine, which have shown significant anticancer activity. Vinblastine treats Hodgkin's disease and choriocarcinoma, while vincristine is effective against pediatric leukemia. Catharanthus roseus also plays a role in traditional medicine across various cultures, treating conditions such as dysentery, diabetes, asthma, and cancer. The plant's bioactive compounds, particularly vinblastine and vincristine, are critical in cancer treatment. Recent nanotechnology advancements could further enhance these compounds' efficacy, paving the way for new cancer treatments. Despite some toxicity concerns, vinca alkaloids remain among the most widely used cancer drugs.

Shreya J Poojari   Sujatha P Muchalambe   Hindustan Abdul Ahad   Aiswarya Sasindran   and Mahalakshmi R.   

Nanosuspensions (NSs) are systems of colloidal particles that are nanoscale in size. This paper investigates how the characteristics of NSs are impacted by formulation and process conditions, as well as underlines current developments, new methodologies, and helpful advice for adapting NSs to diverse routes of administration. In the field of nanomedicine, they have quickly become one of the most fascinating materials. The low solubility of certain drug molecules poses a significant issue in formulating drugs. Drug NSs have arisen as a potential way to administer hydrophobic drugs. Reducing nanoparticles boosts drug solubility and availability in water by expanding the drug's surface area that interacts with biological fluids. NSs stabilized by steric polymers, such as polyethylene glycol (PEG), and ranging in size from 10 to 100 nm, are of special significance. With little collateral damage to healthy tissues, these nanoparticles may encircle tumors and infarct zones. Some commercially available nanosuspension methods include top-down and bottom-up procedures, media milling, emulsification, melt emulsification, high-pressure homogenization, and emulsification. Additional methods used to improve certain properties in advanced treatments include solidification and surface modification procedures performed after production. This review will first discuss techniques for preparing NSs. In conclusion, we emphasize common methods of character portrayal and various practical applications for designing drug delivery systems and utilizing different routes of administration including, pulmonary, parenteral, oral, and ocular routes.

Siddhartha Sankar Das   Hiyashree Sharmah   Arupjyoti Das   Dipjyoti Sharma   Bhargab J Sahariah   Manish Majumder   and Koushik Nandan Dutta   

A major worldwide problem, antimicrobial resistance calls for new natural medicinal agents to be found. The ethanolic leaf extract of the traditionally used medicinal herb Nymphaea rubra is the subject of this investigation, which aims to discover bioactive components and assess their antibacterial capabilities. Based on their statistically significant peak area percentages, 17 of the 80 phytochemical substances identified by Gas Chromatography-Mass Spectrometry (GC-MS) study were chosen for additional investigation. Some of the many bioactivities displayed by these chemicals include antibacterial, antioxidant, and anti-inflammatory capabilities. Proteins from Staphylococcus aureus and Escherichia coli were the targets of molecular docking investigations, which showed strong binding affinities. With binding scores of -8.9 kcal/mol for S. aureus and -7.2 kcal/mol for E. coli, respectively, 10-Methoxy-nb-alpha-methylcorynantheol and Geranyl linalool isomer B were the compounds that performed the best among those that were studied. Significant inhibitory zones against E. coli and S. aureus were observed at doses of 10 µg/mL and 20 µg/mL, respectively, in the in vitro antibacterial activity evaluated using the agar well diffusion method. It was shown that for both bacterial species, the extract had a minimum inhibitory concentration (MIC) of 250 µg/mL. N. rubra may contain bioactive chemicals that can fight against bacteria and viruses that are resistant to drugs, according to these results. Building on previous research into the phytochemical profile and antibacterial activity of N. rubra, this study lays the groundwork for future research into antimicrobial drugs derived from plants. There are real-world consequences, such as the possibility of developing natural antibacterial treatments to deal with public and clinical health issues. To properly appreciate N. rubra's medicinal potential, future studies should investigate in vivo validation and clinical applications.

Ashish Tale   Balaji Thakare   Shirish Jain   and Sachin Borikar   

Background: The current study aims to investigate the analgesic and antioxidant activity of ergocalciferol. Tissues contain vitamin D receptors that help to maintain homeostasis. The objective of this research is to eliminate the adverse effects of drugs that are currently on the market. Methods: This prospective experimental study employed healthy albino mice with IAEC approval. Mice were divided into five groups such as Control group received normal saline, Standard group received morphine 1mg/kg and test group received ergocalciferol at doses of manner like 0.015, 0.03, and 0.06 mg/kg/mice. After treatment, behavioral analysis was carried out for the assessment of central and peripheral analgesic effects using hot plate and tail flick analgesiometers, tail immersion and acetic acid-induced writhing as a well validated animal model for screening of the analgesic effect of drug in a preclinical laboratory. After the writhing test, all animals were sacrificed and screened for oxidative stress markers and antioxidants. Results: At 30–240 min, the test dose of 0.06 mg/kg notably prolonged response time in the hot plate test and tail flick test. Moreover, in the tail immersion method, ergocalciferol at 0.06 mg/kg notably increases tail elongation reaction time to 30–240 min. In the acetic acid writhing test, ergocalciferol at 0.06 mg/kg dramatically inhibits the writhing behavior in experimental animals. Moreover, test drug ergocalciferol at the dose of 0.03 and 0.06 mg/kg restored SOD and GSH levels and conversely found to reduce elevated LPO levels. Conclusion: Ergocalciferol shows central and peripheral analgesic effects, possibly due to its antioxidant potential. Extensive animal study is needed to understand the mechanistic approach.

Jaspreet Kaur   and Indu Melkani   

There is no doubt that a few researchers have contributed to discovering secret medicinal possibilities in ayurvedic medicine, but there are still many plants that require extensive research. A variety of herbal remedies are used in the treatment of ayurveda herbs for the treatment of dementia, and recent studies indicate that they have memory-enhancing properties. Nowadays, liquorice is the most widely used commercial flowering plant herb. It is also used in cuisine, candy, nicotine goods, cough syrups, and snuff flavors. The different functional processes that liquorice and its related chemicals exhibit are responsible for their diverse pharmacological activities, and liquorice's beneficial properties can be linked to several different processes. Liquorice is a plant scientifically known as Glycyrrhiza glabra. The roots and rhizomes of Glycyrrhiza glabra are thought to be an excellent brain tonic because they improve the circulation of the CNS system and blood sugar levels. Glycyrrhiza glabra is a common herb derived from the family Fabaceae (also known as Leguminosae), native to Eurasia, North Africa, and Western Asia. Several compounds found in this plant, which include glycyrrhizin, glycyrrhizinic acid, isoliquiritin, and glycyrrhizic acid, have been identified as neurological, anti-cancer, anti-atherogenic, anti-diabetic, anti-asthmatic, anti-inflammatory, anti-microbial, antispasmodic, Hepatoprotective , immunologic components. They have anti-depressants, sedatives, and anticoagulant properties, as well as the ability to increase hair growth and control weight. This article reviews the latest research on phytochemical and pharmacological data, as well as liquorice and its adverse effects on its bioactive and toxic components.

Aishwarya Bindenahalli Mohan Kumar   Syed Sagheer Ahmed   Bharathi Doddla Ragunathnaidu   Chandan Komalkumar   and Jayanth Baburayanakoppal Manchegowda   

Rheumatoid arthritis (RA) leads to joint deterioration and inflammation, causing pain and disability. Traditional therapies like Non-steroidal anti-inflammatory drugs (NSAIDs), Disease-modifying antirheumatic drugs (DMARDs), and biological products have limitations and adverse effects, prompting interest in complementary treatments like phytosomes. Phytosomes enhance the bioavailability of plant-derived chemicals by combining them with phospholipids. Substances like curcumin, boswellic acids and EGCG exhibit anti-inflammatory and antioxidant properties relevant to RA. Phytosomal formulations of these compounds show increased effectiveness compared to conventional forms. Curcumin and boswellic acids in phytosomal form demonstrate anti-inflammatory and cartilage-protective benefits in RA models. Epigallocatechin-3-gallate (EGCG) from green tea, when phytosomally delivered, reduces inflammatory mediator release and aids in joint tissue healing. Moreover, phytosomal formulations may reduce systemic toxicity associated with traditional RA treatments, crucial for managing the disease's chronic nature. Phytosomes may modulate the immune system, impacting cytokine production and immune cell activity, potentially modifying the disease course. Despite promising preclinical and some clinical data, further randomized controlled studies are needed to confirm the safety and efficacy of phytosomal treatments for RA. Personalized treatment regimens and evaluation of herb-drug interactions are vital considerations. Hence, phytosomes offer improved bioavailability and therapeutic potential for plant-derived compounds in RA therapy. However, a comprehensive understanding of their mechanisms, dosage optimization, and long-term safety necessitates further research. Integrating phytosomes into RA care could provide patients with additional options for symptom relief and enhanced quality of life.

Peter De Roux Sumer   Loushambam Samananda Singh   Bimal Debbarma   Kmensiful Binan   and Waibiangki Lyngdoh   

The primary goal of a drug delivery system is to transport drugs to their intended locations. Researchers have utilized various polymers to create nanoparticles that enhance the therapeutic effects of drugs while minimizing toxicity levels. Chitosan, a natural polymer derived from chitin, is commonly used in this process. Chitosan is obtained by removing its acetyl groups and possesses several desirable characteristics for drug delivery, such as being non-toxic, biodegradable, eco-friendly, and anti-inflammatory. This review aims to explore the creation of chitosan nanoparticles (ChNPs) using different preparation methods, examine the challenges associated with using ChNPs for various purposes, and investigate their potential in the medical field. Advanced gelation methods, such as ionotropic gelation, microemulsion, and emulsification solvent diffusion techniques, are highly efficient for generating ChNPs. Chitosan nanoparticles have the advantage of being able to encapsulate and regulate drug release, particularly in acidic aqueous environments. This review also delves into the biodegradability and toxicity of chitosan and discusses the properties of nanospheres that make them promising for targeted drug delivery to specific areas of the body. In conclusion, this study contributes significantly to the ongoing effort to develop more advanced drug delivery approaches that address the limitations of current methods.

Abhijit Salokhe   Panchaxari Dandagi   Sujay Hulyalkar   and Krutuja Chougule   

Aim: The current study aims to formulate ethosomal gel loaded with serratiopeptidase to improve bioavailability and reduce systemic side effects. Methods: An ethosomal gel formulation loaded with serratiopeptidase was developed, optimized, and evaluated to facilitate topical drug delivery for enhanced therapeutic efficacy. Ethosomes were prepared using ethanol injection technique and 3² factorial design was used for optimization. Nine distinct ethosomal formulations with two different concentrations of soya lecithin and ethanol were evaluated for their % entrapment efficiency, vesicle size, drug content, and zeta potential. The optimized ethosomal formulations were mixed into the gelling base containing Carbopol 934(1%), triethanolamine and methylparaben. The drug content, viscosity, pH, spreadability and in-vitro drug release study employing Franz diffusion cell were further assessed for the generated ethosomal gel. Results: The optimized serratiopeptidase loaded ethosomal formulation F6 with Ethanol: Soya lecithin ratio of (0:1) showed a low vesicle size 158.6nm, % entrapment efficiency of 86.58 % and ZP was found to be -18.1 and PDI was 0.306. The cumulative present release of optimized ethosomal gel (F6) was shown the maximum release was found to be 79.10. TEM analyses for ethosomes nanoparticles were identified to be in spherical shape. On the basis of obtained results of serratiopeptidase loaded ethosomes, gel was formulated by incorporation of optimized formulation F6 into gel base. The gel of serratiopeptidase-loaded ethosomes was prepared by utilizing carbopol 934. The viscosity was found to be 1742±1.20, spreadability 4.3±0.11 and pH 6.32±0.12. The SRP formulation was found to be stable too as per ICH guidelines. Conclusion: The study was successfully completed, focusing on formulating serratiopeptidase-loaded ethosomes for topical delivery to minimize oral side effects and improve drug bioavailability. This approach presents a more effective option for drug delivery through the topical route.

Babiker Bashir Haroun Baraka   Kalavati Jambigi   Niranjan R   Suhas Gowda H D   Santhosh G   and Pradeep L   

Purpose: This study's objective was to have a thorough grasp of patient profiles, Quality of life and related risk factors in individuals with diabetes, to improve clinical pharmacy services and diabetes management. Methodology: The study recruited 107 diabetes participants, collecting data through surveys, interviews, medication histories, and laboratory results. Patients with type 1 or type 2 diabetes who were above 18 and had been exposed to diabetes for more than two years met the inclusion criteria. The Pranav Diabetes Center Ethics Committee gave their approval to the project, which was conducted as a prospective, cross-sectional study from November 24, 2023, to January 17, 2024, in Bangalore. Data were analysed using SPSS version 26, employing multivariate logistical regression and a modified WHOQOL-BREF questionnaire. Results: The study included 107 participants (52 males, 55 females). Most were over 46, married, urban residents, non-smokers, and non-drinkers. 62% were non-working. Blood sugar levels varied, showing diverse glycemic control. Metformin was the most prescribed medication (61.4%), followed by insulin (9.8%). Diabetes affected work efficiency, physical health, and personal relationship satisfaction. Conclusion: The study highlights the diverse profiles and challenges faced by diabetic patients. Regular monitoring and tailored medication regimens are essential for effective management. An improving understanding of patient-specific factors can enhance care and outcomes. Major Contribution to the Field: This research provides important new understandings of the clinical and demographic characteristics of patients with diabetes, emphasizing the need for individualized care approaches and regular monitoring to improve diabetes management and patient Quality of life.

M. Ganga Raju   P. Manasa   N. V. L. V. Suvarchala Reddy   G. Kaveri   and B. Archana   

Diabetes mellitus (DM) is the most common metabolic and endocrine disorder; it is characterized by an absolute decrease in insulin secretion. Nevertheless, there are additional factors in the pathophysiology of diabetes mellitus, such as elevated glucagon secretion, decreased renal glomerular glucose absorption, insulin resistance in adipocytes, and dysfunction of neurotransmitters. Although a variety of therapies are currently available for glycemic control, managing diabetes mellitus is still challenging and complex due to the determination of many pathogenic factors that contribute to the illness. Today's DM therapeutic interventions primarily target glucose control; however, they fail to take into account additional pathological elements that ultimately cause treatment failure and DM progression. Moreover, prolonged use of these commercially available anti-diabetic medications causes a variety of side effects, which is why scientists are always looking for novel anti-DM medications. These innovative therapeutic approaches target both alternating and multiple pathogenic hotspots linked to diabetes mellitus (DM), according to numerous international studies. The current review article discusses both potential side effects from the use of these novel candidate drugs and novel therapeutic options that hold particular promise for ensuring their safety. This will help to successfully develop these drugs into potentially effective medications for the treatment of diabetes mellitus.

Komal Patel   Krutika Poshiya   and Vaibhavkumar Patel   

Amoxycillin trihydrate, cloxacillin trihydrate and probencid are proven for their therapeutic benefits to treat bacterial infection. There are numerous approaches available for the simultaneous estimation of two medicines, but there is none accessible for the estimation of three medications, or the ones that exist are quite complicated, so the current study focuses on developing and validates a new, simple, rapid and novel spectrophotometric method for simultaneously estimating amoxicillin trihydrate, cloxacillin sodium, and probenecid in pure and solid dose forms using the simultaneous equation method. The λmax of Amoxicillin Trihydrate (AMOX) (10 μg/ml), Cloxacillin Sodium (CLOX) (10 μg/ml), and Probenecid (PROB) (10 μg/ml) were 279.89 nm, 219.02 nm, and 239.67 nm, respectively. The medications followed Beer's rule and showed a good connection. Calibration curves for AMOX, CLOX, and PROB were linear from 5 to 30 μg/ml. The results indicated that the technique was accurate, precise, and reproducible (with a relative standard deviation of less than 1%) as per ICH guidelines. It is also affordable, simple to use, and time-saving, making it appropriate for the simultaneous determination of three medicines in commercial preparations. The proposed methods are recommended for routine analysis since they are rapid, simple, accurate, cost effective and also sensitive and specific. It involves neither heating nor use of any organic solvent for separation of the combination. Thus, this study exploits the possibility for determining Pharmacokinetic data of the combined formulation which may be required in pre-clinical and clinical studies in near future.

Preeti Lakra   Aarti Tiwari   Gulshan Athbhaiya   Rajesh Choudhary   and Pradeep Kumar Samal   

This research is designed to assess the anti-atherogenic activity of aminoguanidine against diabetes-accelerated atherosclerosis in albino rats. The Wistar albino rats (150-200 g) were used for the investigation. Animals were fed an atherogenic diet for 45 days after by acute intraperitoneal injection of alloxan (120 mg/kg) on the 0th day. From day 16th to 45th, group II (atherogenic control) received normal saline (10 ml/kg/day, p.o.), group III (standard) received atorvastatin (10 mg/kg/day, p.o.), group IV (aminoguanidine-25) received intraperitoneal injections of aminoguanidine at a dose 25 mg/kg/day, and group V (aminoguanidine-50) received intraperitoneal injections of aminoguanidine at a dose 50 mg/kg/day. The results showed the potential beneficial effect on aminoguanidine-treated animals especially at 50 mg/kg dose level, when compared to the atherogenic control group. Aminoguanidine treatments significantly restore the body weight, serum lipid levels (total cholesterol, triglycerides, LDL, VLDL, and HDL), atherogenic index, and serum hepatic biomarkers (aspartate aminotransferase, alanine aminotransferase, and alkaline phosphate). Moreover, results showed the potent antioxidant activity of aminoguanidine, which is indicated by significant restoration in hepatic oxidative stress markers like catalase, reduced glutathione, malonaldehyde, and nitrite content in the aminoguanidine treatment group. Overall results conclude that aminoguanidine mitigates the progression of atherosclerosis against diabetes-accelerated atherosclerotic animal model by its potent antihyperlipidemic and antiatherogenic activity.

Sankara Rao Miditana   Saivenkatesh Korlam   A. Ramesh Babu   V. Prabhakar Rao   and M. Aruna Kumari   

Nicotine, a potent alkaloid present in tobacco, is well-known for its highly addictive nature and significant health hazards, such as cancer, heart disease, and respiratory diseases. This review delves into nicotine's comprehensive impact on various biological systems and overall health. It provides a detailed examination of nicotine's detrimental effects on the brain, cardiovascular, respiratory, immune, and reproductive systems, alongside its profound implications for mental health. Despite its well-documented adverse effects, emerging research highlights potential cognitive benefits of nicotine in neurodegenerative conditions such as Parkinson's and Alzheimer's diseases. Specifically, nicotine has demonstrated promise in improving cognitive function in Alzheimer's disease and alleviating dyskinesia and memory problems in Parkinson's disease. These therapeutic effects are thought to be mediated through mechanisms involving Sirtuin 6 inhibition, enhanced protein kinase B activity, and stimulation of phosphoinositide 3-kinase/Akt signaling pathways. Furthermore, this review explores the dual nature of nicotine's impact, emphasizing both its severe health risks and its potential therapeutic benefits, particularly in the context of cognitive disorders. The analysis aims to provide a balanced perspective on nicotine, acknowledging its harmful consequences while also considering its possible utility in specific medical scenarios. Understanding these complex dynamics is crucial for developing effective public health strategies and therapeutic interventions that can mitigate nicotine's risks while potentially harnessing its benefits for treating neurodegenerative diseases. Such a nuanced approach is essential for informing public health policies and advancing therapeutic research, ultimately contributing to improved health outcomes.

Sadishkumar S.   Prathiba R.   Mohith SN   Abilash S.   and Vimal Kumar S.   

Erectile dysfunction (ED) is one of the most common sexual disorders in men which occurs due to various biological, environment and rarely genetic factors. The study is conducted due to various side effects of the currently available erectile dysfunction drugs such as PDE 5 inhibitor. The objective of the study is to evaluate the aphrodisiac activity of Fragaria ananassa fruit extract in drug-induced erectile dysfunction in rats. The fruit of Fragaria ananassa was extracted by the hydroalcoholic extraction method and evaluated for its preliminary phytochemical investigation and further molecular docking studies were carried out. The hydroalcoholic extract of the fruit at different doses (500mg/kg and 1000mg/kg) is used for in vivo studies carried out in rats and various physical mating parameters, serum testosterones, FSH, LH, AST, ALT, TC, and antioxidant SOD, CAT and LPO were estimated along with the histopathology studies and compared with standard sildenafil (4.5mg/kg). The phytochemicals screening confirms the presence of the flavonoids, glycosides, phenols, in Fragaria ananassa fruit extract (FAFE). In metronidazole induced model, FAFE shows a significant effect against dysfunction by improving the serum hormonal levels and restoration of the natural antioxidant system (SOD, CAT & LPO) and histology of the testis, which serves as evidence for the aphrodisiac activity of FAFE. From the present study, it can be concluded that the hydroalcoholic extract of Fragaria ananassa fruit extract (FAFE) possesses aphrodisiac activity and enhances erection. FAFE is effective in ameliorating the effects of metronidazole induced ED model in rats.

Vandna Choudhary   Shilpa Sharma   Amita Malik   Alankar Shrivastav   and Pawan Kumar Shukla   

Purpose: The study aimed to evaluate the wound-healing efficacy of an ethanolic extract of Calendula officinalis flower petals, traditionally used by tribal communities. This extract was encapsulated in hydrogels made from modified okra mucilage and acrylic acid to enhance its therapeutic effects. Methods: Mature flower petals of Calendula officinalis were crushed to prepare an ethanolic extract. This extract was encapsulated in hydrogels and applied to excision wounds on animal models. A comparative analysis was conducted on encapsulated and unencapsulated hydrogels. Epithelization period, contraction area, hydroxyproline content, total protein, antioxidant activity, wound index and histopathological evaluations were among the key parameters analyzed. Results: The study revealed that animals treated with encapsulated hydrogels demonstrated significantly improved wound healing outcomes compared to those treated with unencapsulated hydrogels and control groups. Specifically, the encapsulated hydrogels led to greater wound contraction, a shorter epithelization period, and a lower wound index. Additionally, higher levels of hydroxyproline, total protein, and DNA concentrations were observed in healing tissue, indicating enhanced collagen synthesis and tissue regeneration. Histopathological evaluations supported these findings with more organized and mature tissue formation. Conclusion: The encapsulated hydrogel of Calendula officinalis ethanolic extract proved to be more effective in promoting wound healing than the unencapsulated versions. This novel hydrogel formulation shows promise as a potent pharmaceutical candidate for acute cutaneous wound care.

KasimMuhtari   Inampudi Sailaja   Beena Kanwar Shekhawat   Sonia Kaura   and Jonwal Harshita   

Endophytic microbes harbored by medicinal plants cooperatively synthesize significant pharmaceutical metabolites in their host plant. The study is aimed to delve into bacterial endophytes of Mangifera indica, Psidium guajava, Cassia occidentalis, Calotropis procera, and Hibiscus roasa-sinensa, by identifying the important industrial enzymes they produce. Surface sterilization was achieved using ethanol, sodium hypochlorite and mercuric chloride as decontaminants. The isolates were identified based on the physiological and biochemical features they express. Then, various screening methods like Carboxymethyl cellulose, tributyrin, Carboxymethyl cellulopectinse, starch, and skim milk agar were used to screen out the strains with the ability to form a halo zone surrounding the grown culture on the agar plate as amylase, cellulase, protease, lipase, and pectinase enzymes producers. And finally, the qualitative assay of the screen isolates was performed according to the enzymes needed to be assayed, e.g., DNS method using starch as substrate for amylase, DNS using glucose as substrate cellulase, caseinase assay method for protease, DNS method for pectinase and titrimetric determination of the free fatty acids for lipase. 30 bacterial strains were isolated, more than 50% of the isolates have shown presence of cellulase, protease, pectinase and lipase as indicated by the halo zone and the whole isolates were expressed to be amylase producers except one. The Quantitative assay of the positive amylase and cellulase isolates detailed low activity while lipase, protease and pectinase positive isolates showed high activity. The study remarks that bacterial endophytes residing in five medicinal plants in this work are producers of essential metabolites applicable in pharmaceutics, medicine and agriculture.

Tejaswini Ullakula   Vani Mathakala   Umamaheshwari Amineni   Umakanth Naik Vankadoth   and Uma Maheshwari Devi Palempalli   

In the present study, two marine brown algae namely Sargassum vulgare, Sargassum longifolium and red algae Gracilaria cearensis were screened for their anti-inflammatory and anti-oxidant activity. The anti-inflammatory activity of algal samples was measured through the inhibition of haemolysis induced by heat and hyposaline. DPPH radical scavenging assay and hydrogen peroxide scavenging assay were adopted to detect the anti-oxidant potential of algal samples. Among the three marine algae, G.cearensis exhibited potential anti-inflammatory and anti-oxidant activity. GC-MS analysis was followed to capture the phytochemical picture of G.cearensis. The detected bioactive ligands were docked with inflammatory proteins such as COX-2, 5-LOX, mPGES-1, iNOS, TNF-α and NF-κB using Maestro 13.0 module of Schrodinger. The standard diclofenac exhibited docking affinity of -3.597 kcal/mol and -2.262 kcal/mol with the protein receptors COX-2 and 5-LOX respectively. While among all the bioactive compounds, 4-methyl-3-heptanone (dialkyl ketone) showed the highest docking energy of -6.608 kcal/mol and -4.205 kcal/mol with COX-2 and 5-LOX receptors respectively. Overall the bioactive ligands namely beta-sitosterol acetate, 4-methyl-3-heptanone, diacetone alcohol and 1-allyl-1,2-cyclohexanediol demonstrated potential binding affinity with the inflammatory markers. Thus the results state that Gracilaria cearensis exhibit dual inhibition against COX-2 and 5-LOX and can be used to develop novel anti-inflammatory drugs.

Kalaivani Madhavaram Kuppusamy   Cordelia Mano John   Bhavana Jonnalagadda   Yadav Sangeeta Muthyalaiah   and Sumathy Arockiasamy   

The current study aimed to understand the effect of Ferulic acid (FA), a phenolic compound with effective antioxidant properties on Tacrolimus (TAC) induced nephrotoxicity in MDCK cell lines. The distal tubular epithelial cell line, MDCK cells were tested for toxicity of TAC and FA using cell viability assay (MTT assay) and the apoptotic and necrotic morphology of cells were studied with AO/EB staining. The cell cycle arrest in TAC and FA co-treated cells was studied using flow cytometry. ROS level was measured using fluorogenic dye, 2,7-dichlorodihydrofluorescein diacetate (DCF-DA) and analysed by flow cytometry. The antioxidant analysis was performed by estimating GSH using 5,5-dithio-bis (2-nitrobenzoic acid) (Ellman's reagent, DTNB) and SOD was measured by the modified NBT method. TAC treated cells showed reduced cell viability, increased apoptosis with cell cycle arrest at S phase and sub G0/G1 phase cell population. But, FA co-treatment significantly (<0.001) increased cell viability with reduced apoptosis. Increased ROS generation, estimated by DCFH-DA in TAC treated cells, was comparatively reduced (<0.0001) in FA co-treated cells with concurrent increase in Glutathione (GSH) (<0.001) and Superoxide dismutase (SOD) (<0.0001) level in FA co-treated groups, which could be attributed to its maintenance of intracellular redox balance. Thus, the maintenance of antioxidant defence status along with free radial scavenging property of FA may provide an adjuvant therapy to reduce the nephrotoxicity induced by TAC.

Pameshwar Kumar   Aarti Tiwari   Gulshan Athbhaiya   and Pradeep Kumar Samal   

This study aims to investigate the hypolipidemic effects of an aqueous extract from the leaves of Raphanus sativus var. longipinnatus using rat models. Hyperlipidaemia, a condition caused by a high-fat diet, was produced in Wistar albino rats through the continuous administration of such food. During this period, weight growth and changes to the serum lipid profile were observed. It specifically indicated a reduction in high-density lipoprotein levels and an increase in total cholesterol (185±0.96), triglycerides (281±1.2), low-density lipoprotein (123±2.0), and very low-density lipoprotein (57±1.4). Atorvastatin administered at a dosage of 10 mg/kg served as the reference medication for the standardisation process. Following a 14-day testing period, rats administered 300 mg/kg of leaf extract exhibited a significant alteration in their weight. A significant increase (P<0.001) was observed in total cholesterol, triglycerides, low-density lipoprotein, and very low-density lipoprotein after the administration of the 300 mg/kg dosage. The quantity of high-density lipoprotein significantly increased (P<0.001) with the 200 mg/kg dosage. Microscopic examination of the liver elucidates the alterations that transpire in hepatic cells throughout the course of treatment. The leaf extract exhibited a notable reduction in oxidative stress markers, along with decreased SGOT and SGPT levels. Comprehensive studies demonstrate that the use of the leaf extract resulted in weight gain and an improved lipid profile in the blood stream.

Chinedu Enegide   Adaobi C. Ezike   Solomon F. Ameh   Ifeoma C. Ezenyi   Samuel E. Okhale   and Peter A. Akah   

Background: Disorders that interfere with the structural architecture and/or functional integrity of the central nervous system are generally described as central nervous system (CNS) disorders. Among the different types of CNS disorders are anxiety and seizure. Though a number of drug classes are currently available for the management of anxiety and epilepsy, different adverse effects and tolerance characterize the use of most of these agents especially after prolonged usage. This thus necessitates research aimed at developing newer agents with fewer adverse effects. Aim/objective: This study aims to evaluate the anxiolytic and anti-epileptogenic activities of . nigricans leaf extract using acknowledged mice models. Materials and method: In the study, identification of bioactive constituents present in CNEE was carried-out using GC-MS analysis. Anxiolytic effect was evaluated using open field test (OFT), elevated plus maze (EPM) and light/dark box (LDB) models. Anti-epileptogenic effect was assessed using pentylenetetrazole (PTZ) induced seizure, while effect on motor co-ordination was assessed using a rotarod apparatus. All pharmacological assessment was carried-out in mice with graded CNEE doses of 200 to 800 mg/kg. Result: Chromatographic analysis of CNEE using GC-MS shows the presence of 34 constituents including phytol. In the three models used to evaluate the anxiolytic effect, CNEE had a significant (<0.001) effect at 200 mg/kg. The extract increased time spent in light compartment in LDB model, increased time spent in open arm in EPM model and also increased the number of center square transverse in the OFT model. In PTZ-induced seizure, it delayed onset of seizure and also increased survival time. The extract did not however affect motor coordination in rotarod test. Conclusion: The study outcome revealed that . nigricans leaf ethanolic extract has the potential for eliciting potent anxiolytic and anti-epileptogenic effects as shown in the animal models used for the study.

Sonali Phule   Aishwarya Jadhav   and Vasant Lokhande   

Hepatotoxicity, characterized by liver damage due to various agents, poses a significant health challenge worldwide. Silibinin (SB), a flavonolignan extracted from the milk thistle (Silybum marianum), has garnered attention for its potential hepatoprotective properties. This review provides a thorough examination of SB's efficacy in mitigating hepatotoxicity induced by drugs, chemicals, metals and toxins. SB's anti-inflammatory properties extend beyond just inhibiting reactive oxygen species. It also encompasses effects mediated by nuclear RNA/DNA, which work to suppress NF-κB binding and translocation. SB demonstrates notable efficacy in countering drug-induced hepatotoxicity, inhibiting tumor necrosis factor α (TNF) expression and associated apoptotic pathways. Moreover, it attenuates the impact of chemical insults, exemplified by its ability to suppress TNF and interleukin 4 expressions in acute hepatitis models. SB's influence on the leukotriene formation and 5-lipooxygenase (LOX) pathway, as well as its inhibitory effects on inducible nitric oxide synthase expression, further contributes to its protective role against various chemical-induced hepatotoxic insults. This comprehensive review synthesizes current knowledge on SB's protective effects in hepatotoxicity, providing insights into its potential as a therapeutic agent against diverse challenges posed by drug, chemical, and metal-induced liver damage. The multifaceted actions of SB underscore its promise as a versatile and effective intervention in the realm of hepatoprotection.

Mazzura Wan Chik   Meor Mohd Redzuan Meor Mohd Affandi   Hanish Singh Jayasingh Chellammal   Nurul Aqmar Mohd Nor Hazalin   and Gurmeet Kaur Surindar Singh   

Astaxanthin, a ketocarotenoid compound belonging to the xanthophyll class, has shown potent antioxidant characteristics when compared to other antioxidants. It has been widely studied and used in in vivo and in vitro models for its biological activity against diseases such as cancer, diabetes, Alzheimer's disease, and skin disease due to its antioxidant ability to combat the oxidative stress that causes inflammation. However, its lipid-soluble nature has limited its clinical applicability due to low oral bioavailability. Astaxanthin in the form of nanoemulsions and nanoparticles demonstrated better oral bioavailability, more stability, and higher cell penetration. Despite their superior properties, the use of astaxanthin nanoemulsions and nanoparticles in pre-clinical animal models for treating various chronic diseases remains limited. Four different databases, including PubMed, Web of Science, Scopus, and Science Direct, were searched using the keywords �astaxanthin nanoemulsion' OR �astaxanthin nanoparticles' AND �disease' to find research journals for this review. The term �disease' was replaced with the names of specific diseases such as cancer, brain disorder, stress, diabetes, and liver disease. This review focuses on recent developments in the use of astaxanthin nanoemulsions and nanoparticles in chronic disease management, and it is expected to be useful for future research.

Kuchi Manjeera   and Raja Sundararajan   

Numerous diseases, such as cancer, diabetes mellitus, aging, arthritis are linked to free radicals. Antioxidant therapy has become increasingly important in the management of several illnesses. Diabetes mellitus is an intricate metabolic ailment characterized by insistent hyperglycemia that interferes with protein, lipid and carbohydrate metabolism. Therefore, using a variety of conventional in vitro models, a modern investigation sought to investigate the antioxidant and antidiabetic properties of Indigofera prostrata. The methanol extracts of Indigofera prostrata were assessed in this endeavor for their ability to block radicals via the use of superoxide radical action, DPPH, lipid peroxidation assay, and the nitric oxide method. Numerous factors, including glucose diffusion, the inhibitory actions of alpha amylase, alpha glucosidase, and the ability of yeast cells to absorb glucose, were also used to measure the in vitro antidiabetic efficacy. When compared to conventional antioxidants, the revealed results of plant extracts demonstrated a higher capability for radical scavenging in relation to their antioxidant activity. Similarly, a variety of characteristics demonstrated that in vitro extracts of Indigofera prostrata had excellent antidiabetic action. In summary, Indigofera prostrata has strong anti-oxidant and antidiabetic qualities.

Duygu Alpaslan   Tuba Ersen Dudu   Abdullah Turan   and Nahit Aktas   

Controlled release systems used in the biomedical industry or still in the animal testing phase generally use various chemicals, especially natural or artificial polymers. In recent years, there has been increasing interest in plant-based products as controlled release materials. For the first time in the literature, poly(apigenin) hydrogel was synthesized from apigenin, an important flavonoid. Swelling percentages and biodegradation percentages of poly(apigenin) hydrogel at different pH values were investigated. Structural analyses of poly(apigenin) hydrogel were performed using FT-IR (Fourier Transform Infrared Spectroscopy). To examine drug release amounts and kinetics, different drug active ingredients (paracetamol, ceftriaxone, and 5-Fluorouracil(5-fu)) were loaded into the poly(apigenin) hydrogel. The release of paracetamol, ceftriaxone, and 5-fu from the synthesized poly(apigenin) hydrogel was determined as 95%, 58% and 96%, (pH 7.4) respectively. For kinetic studies, zero-order, first-order, Higuchi, and Korsmeyer-Peppas, models were used. When the correlation coefficients (R²) were compared, it was seen that the drug release kinetics fit better with the Korsmeyer-Peppas model. It was observed that the poly(apigenin) hydrogel synthesized in this study was a suitable material for the release systems of paracetamol, ceftriaxone, and 5-Fluorouracil.

Shilpa Rana   Uddipak Rai   Vineet Kumar   and Mansi Butola   

Background: Globally, breast cancer is the most common malignancy in women and the second most common cause of cancer-related death among women. There is therefore a need to identify more efficacious therapies for this neoplasm. Therapeutic treatment of liver cancer has been also a great challenge. Use of herbal drugs in treatment of cancer has been a great choice for the researcher. Eupatorium adenophorum also known as Ageratina adenophora belongs to the family Asteraceae which is a new plant found with anti-cancer properties. Methodology: The successive extraction of the leaves was carried out using Petroleum ether (PET), Chloroform (CHCl₃) and Methanol (MeOH). The three extracts obtained were carried out for anti-cancer activity via 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay on breast cancer cell lines (MDA- MB-231) and liver cancer cell lines (HepG2). Result: Best anti-cancer activity was found in PET and MeOH extract in HepG2 and MDA-MB-231 cell lines respectively. Further characterization was carried out via Liquid Chromatography-Mass Spectroscopy (LCMS) in order to identify the chemical constituents responsible for anti-cancer activity. Conclusion: The LCMS data confirmed the presence of chemicals from polyphenol and flavonoid and fattyacid category in MeOH and PET extracts which could be responsible for inhibiting the viable cancer cells. This study indicates that MeOH and PET have better anti-cancer activity. So Eupatorium adenophorum can be the greater choice for the researcher in the treatment of cancer.

Mansi Patel   Tanvi Dodiya   and Disha Prajapati   

Forskolin, classified as a labdane-diterpenoid, exhibits the remarkable ability to stimulate vital cellular enzyme adenylyl cyclase, which triggers elevated levels of the critical secondary messenger molecule cyclic AMP across various cell types. This bioactive compound occurs naturally in the roots of Coleus forskohlii, a distinguished member of the mint family Lamiaceae. The plant is commonly known as Indian Coleus, makandi, and pashan bhedi. Various chemical and biological synthesis techniques aim to produce forskolin efficiently and sustainably. The extraction of forskolin is achieved through various techniques, including hydrotropic solubilization, ultrasonication, Soxhlet extraction, microwave-assisted solvent extraction, matrix solid-phase dispersion extraction, and heat reflux extraction using various solvents. Analytical methods for the estimation of forskolin encompass UV-visible spectroscopy, liquid chromatography (LC), high-performance liquid chromatography, thin-layer chromatography (TLC), and high-performance thin-layer chromatography. Additionally, forskolin has garnered attention in clinical and experimental studies, revealing diverse pharmacological effects. These include antiplatelet, bronchodilating, vasodilating, antihypertensive, anticancer, antidiabetic, and antiglaucoma properties. Further research on optimizing extraction methods, testing techniques, improving absorption by the body, as well as understanding the mechanisms of how forskolin acts in the body, could expand its medical uses. The versatile nature of forskolin's pharmacology underscores its potential as a valuable compound in various therapeutic applications.

Poonam A. Sanam   Nayana S. Baste   and Sanjay B. Patil   

The term "fast dissolving oral drug delivery system" refers to a system that dissolves or disintegrates in a matter of seconds or minutes when held in the mouth without water and swallowed. Oral fast dissolving films have emerged as a viable drug delivery technique in recent years, owing to a number of advantages for pediatrics and geriatric patients who have difficulty in swallowing. These little, thin oral film strips are meant to make medicine administration easier when the film is placed on or under the tongue. These films allow the medicine to be delivered directly into the bloodstream via buccal or sublingual routes. Oral films have been shown to improve the onset of action, reduce dosage, and increase bioavailability. This review article discusses the history, benefits, and limitations of oral rapid dissolving films, as well as formulation considerations, manufacturing processes, evaluation parameters, packaging, and marketed products. Due to its unique properties, novel attributes, competitive standing, and cost adequacy, it can be inferred that it is one of the fastest-growing dosage forms with a lot of potential, particularly for commercial applications.

Manikant B Karadesai   Akshay K Patil   Praneeth N Mandi   and Sunil S Jalalpure   

The objective of current research work was to integrate Quality by Design (QbD) approach with the principles of green analytical chemistry with a focus on minimizing detrimental environmental effects. A cost-efficient UV spectroscopic method was developed and validated as per ICH guidelines for chrysin analysis. Water was used as a major solvent. Sonication time and scanning interval were chosen as independent variables and absorbance was selected as dependent variables. DoE was used to optimize trial runs. To identify the optimized spectroscopic method, a simple 3² factorial design with 2 factors and 2 levels was employed, resulting in 9 experimental runs. The optimized run was extensively validated as per ICH guidelines. A linear relationship was determined between the concentrations ranging from 2 to 10 µg/ml, with a regression coefficient of 0.998. Both precision assays showed a % RSD less than 2 indicating the precise nature of the method. The percentage recovery ranged from 99.84 to 101.26% indicating promising accuracy. Sensitivity of the proposed method is proved by its LOD and LOQ values which are 0.51 ÎĽg/mL and 1.57 ÎĽg/mL respectively. The % RSD less than 2 indicates that the developed method is rugged and robust. Additionally, the method exhibited promising repeatability. Hence, it can be concluded that integration of QbD and Green chemistry offers a promising avenue for developing a cost-effective and environment friendly analytical method for chrysin analysis.

Ali Hendi Alghamdi   Reem A. Balol   Aimun A. E. Ahmed   Haidar Abdalgadir   and Mahadi Bashir   

Onion (Allium cepa L.) was mentioned in the holy Quran and the Bible for its importance to ancient civilizations as a food flavor and healing herb. The onion Peels (OP) were traditionally used for various ailments with little data on their safety. The study was set up to determine the acute oral toxicity of the aqueous extract of onion peels in rats, in vivo using Protocol 425. The acute oral toxicity of the aqueous extract of OP was evaluated using the AOT 425 protocol, where the limit test was carried out, after an adaptation period of 7 days, using the 2000 mg/kg mode as a single dose, and a total of 5 rats were used to meet the stopping criteria, then the main test was carried out to estimate the LD₅₀ of the OP extract using the up-and-down procedure guided with software (AOT425ststpgm) and doses of (175, 550 and three 2000 mg/kg) as a single dose. Rats were observed for 14 days. On day fifteen, rats were anesthetized and blood samples were collected from all groups to evaluate the effects of hematological, biochemical, liver, and kidney functions, after euthanization of rats; all main organs were collected in formalin and sent for histopathological investigations. The results revealed that during the adaptation period, the limit group rats exhibited a significant increase in food consumption. The limit test showed normal results concerning general characteristics, hematologic, renal function, histopathological, and biochemical parameters, except reduction in glucose level. On the other hand, the total proteins of the liver increased, while albumin decreased. The main test showed normal results on the general characteristics, hematological, biochemical, renal function, and histopathological characteristics. Liver total protein and liver enzyme ALT increased, while albumin levels decreased. The OP extract has no signs of toxicity and mortality, and its estimated LD₅₀ is higher than 2000 mg/kg. We concluded that the dry onion peel aqueous extract has a wide margin of safety estimated as (LD₅₀), and it was also found to be free of any toxic effects on the histopathology, hematological, renal function, and biochemical parameters of the main organs.

Vidhan Chand Bala   Tahira Sultan   Dinesh Kumar   Sunil Kumar Tiwari   Amit Kumar   and Sushil Kumar   

This research study evaluates the effect of the neuroprotective activity of the dried leaves extract of Amaranthus tricolor (LEAT) on haloperidol causing catalepsy in laboratory rats. The catalepsy is caused by intraperitoneal administration of haloperidol (1mg/kg). The composition of the LEAT extracts at low and high dosages, and the standard drugs being tested were given orally (p.o.) 30 minutes before treatment with haloperidol and catalepsy was measured using behavioral test models. The efficacy and inhibition of catalepsy were calculated by the one-way ANOVA method. According to the findings of the phytochemical screening, the LAT contains flavonoids, saponins, alkaloids, tannins, sterols, amino acids, carbohydrates proteins, &fats. An acute oral toxicity study investigation on the LAT, but not through a report of its toxicity was available. The outcomes demonstrate that the LEAT low dose considerably (p<0.001) decline the catalepsies score after giving haloperidol for 30, 60, 90, 120, 150, and 180 minutes. The catalepsies score was significantly (p<0.001) declined by both standard drug (levodopa 5mg/kg) and LAT high dose in comparison to the disease control group. The levodopa 5mg/kg with LEAT 400mg/kg also significantly (p<0.001) declines the catalepsy score. The research suggested that levodopa-infused LEAT significantly enhanced efficacy in comparison to the disease control group. As a result, the study concludes that A. tricolor combined with levodopa can potentially manage neurodegenerative disease because it affects almost all of the medals.

Jaydeep Patil   Tanvi Dodiya   and Disha Prajapati   

Taxifolin, commonly known as dihydroquercetin, is a plant constituent that belongs to the flavanonol derivates of flavonoids found in Chinese yew, Chir pine, Silybum marianum, Vigna angularis, Cedrus deodara, Larix sibirica etc. The review explores deeply into the steps that enzymes carry out in the synthesis of taxifolin within plants. It can be isolated and extracted from different food products and parts of the plant through different methods such as Ultrasound-Assisted Extraction, Extraction Utilizing Microwave Assistance, Soxhlet extraction, Supercritical fluid extraction, Flash chromatography, High-Speed Countercurrent Chromatography (HSCCC), etc. This review focuses on various techniques involved in the extraction process and analytical methods related to its identification and characterization. Many analytical methods, including HPLC, UPLC, HPLC-MS, and LC-MS, have made it possible to evaluate taxifolin both qualitatively and quantitatively. The compound exhibits diverse applications, including its utilization for antioxidative, antibacterial, anti-acne, tyrosinase inhibition, anti-toxoplasmosis, anti-inflammatory, anti-tubercular, antiviral, anti-Alzheimer, hepatoprotective, osteoclastogenesis and cardioprotective effects. This review adds many new insights to our understanding of taxifolin isolation, analysis, and biological activity, which will be helpful for future research.

Enush Daimari   Uma Dutta   Barnali Haloi   Bhaigyaroti Muchahary   and Trishna Kalita   

N-nitrosodimethylamine (NDMA), the structurally simplest nitrosamine, is a potent carcinogen. Since nitrosamines are found in a broad range of substances, including our water and food, it is important to look for ways to nullify their harmful effects. In this regard, supplementing our diet with plant materials rich in bioactive compounds can be useful. Therefore, this study aimed to study the protective effects of the combined extract of selected plants against the carcinogenic impact of NDMA treatment on mice. Metabolites present in the methanolic extracts of the selected plants were screened. After checking the toxicity of the combined methanolic extract (CME), mice were segregated into four groups, namely control; NDMA-treated; NDMA + CME (200 mg/kg body weight) treated; and NDMA + CME (400 mg/kg body weight) treated. The weight of mice was checked at regular intervals. After the experimental period, the mice were sacrificed which was followed by collection of blood and observation and weighing of the internal organs. The lung, kidney, and liver were fixed in 10% formalin for histopathological examination. Phytochemical screening showed good amounts of important metabolites. The change in body weight of the NDMA-treated group was most distinct from the control group's body weight change. The relative organ weight for liver of different experimental groups significantly differed. NDMA induced hepatocarcinogenesis, renal toxicity, and histopathological injury in the lung. In the case of NDMA + CME-treated mice, normalised histological architecture was observed. This study indicated that the phytoactive components of CME counteracted the toxic effects of NDMA.

Priyanka Arya   Vikram Sharma   Rahul Sagar   and Surabhi Thapliyal   

Impaired brain cholesterol homeostasis has been implicated in the development and progression of Alzheimer's disease (AD). Cholesterol is crucial for various neuronal functions, including synapse formation, neurotransmitter release, and membrane fluidity. Disruptions in cholesterol metabolism can lead to the accumulation of toxic proteins such as beta-amyloid and tau, which are hallmarks of AD pathology. Proprotein convertase subtilisin/kexin type 9 (PCSK9) was initially discovered in the brain, suggesting it may play a role in brain development and cell death. While its exact function in the nervous system and the progression of Alzheimer's disease (AD) remains unclear, PCSK9 is believed to affect neuronal and lipid receptors, such as low-density lipoprotein receptors (LDLR), LDL receptor-related protein 1 (LRP1), and apolipoprotein E (APOE). These effects can lead to decreased cholesterol uptake by neurons and glial cells, disrupting cellular functions and potentially contributing to neurodegeneration and the development of AD. Studies have shown that PCSK9 levels are elevated in the cerebrospinal fluid (CSF) of individuals with AD, suggesting a potential association between PCSK9 and AD pathogenesis. Additionally, evidence highlights that treatment with PCSK9 inhibitors like alirocumab and evolocumab reduces dendritic spine loss via reduction of microglial, astrocytic activation and amyloid β aggregation. Overall, while the exact mechanisms by which PCSK9 influences brain cholesterol homeostasis in AD are still being elucidated, accumulating evidence suggests that PCSK9 may play a role in this process and could represent a potential therapeutic target for AD. Therefore, the present review sheds light on the PCSK9 potential role in the pathogenesis of AD by modulating brain cholesterol homeostasis.

Barkha Devi   and Sonam Zangmu Sherpa   

Introduction: Menstruation, frequently referred to as 'period', is a common phenomenon among women, in which the blood gets discharged from the uterus into cervix and then, passes via the vagina. Dysmenorrhea is one of the most common reasons for the occurrence of menstrual problems as well as pelvic discomfort while it causes painful uterine cramps during menstruation. It is also the most commonly found issue among women, particularly during their reproductive stage. Many research works have determined the effects of supplements containing vitamins E and ginger upon reducing the severity of primary dysmenorrhea. Aims & Objective: The current study is aimed at analyzing the impact of ginger and Vitamin E upon pain severity among adolescent girls enrolled in colleges with primary dysmenorrhea. Further, the study also aims at determining the association between pain scores among the students who consume additional pain relief medicine or therapy during the course of the study. Methods: This non-blinded randomized controlled experiment was carried out for four months in 2022 among the students aged between 18 and 25 years, residing in the hostels of Sikkim Manipal University, Sikkim and experienced moderate to severe dysmenorrhea during menstruation. For this study, a total of 102 students were selected and were randomly segregated into three groups such as control, Vitamin E and ginger power group. With the help of a background questionnaire as well as a pre-tested Visual Analogue Scale (VAS), the author analyzed the impact of ginger power and vit-E upon reducing the severity of primary dysmenorrhea for three successive cycles. The data collected using the questionnaire were analyzed using SPSS version 21. Results: At the beginning, a total of 187 participants were covered for the investigation among which 85 study participants were excluded from the study citing not meeting the inclusion criteria or dropping out from the study. Prior to the intervention, the mean VAS scores of the overall study population for dysmenorrhea were 7.03 (Control group), 7.15 (Ginger group) and 7.00 (Vitamin E group) respectively while after the third month of the trial, the mean VAS scores were calculated as 6.62 (Control group), 4.74 (Ginger group) and 4.47 (Vitamin E group) respectively. Among the groups, vitamin E group respondents mentioned that their pain intensity got heavily reduced (F=32.573, P<0.001), followed by the ginger powder group (F=25.868, P<0.001). Conclusion: The current study findings confirmed that it is possible to significantly reduce the impact of dysmenorrhea by administering ginger powder and vitamin E while the latter shows the maximum impact. Since administering these supplements carries a lower risk in comparison with analgesics, in-depth research is required to validate the findings and determine their effects.

Dhara Trivedi   Kashyap Thummar   Bhumika Maheriya   and Sanjay Chauhan   

Clinical trials are essential investigations that evaluate the safety and effectiveness of new medications, addressing modern health challenges. Typically lasting 10-12 years, these trials assess novel therapies to improve public health outcomes, which are critical in drug discovery. Historical landmarks such as the Nuremberg Code and Declaration of Helsinki set ethical guidelines, while incidents like the thalidomide tragedy prompted regulatory changes like the Kefauver-Harris Amendment, prioritizing safety in drug approvals. Regulations ensure ethical standards, participant safety, and trustworthy data, advancing medical research and patient welfare. India has a comprehensive regulatory framework governing clinical trials, evolving from historical challenges with drug regulation during British rule. Significant changes occurred post-independence, with the establishment of the Drugs and cosmetic act, of 1940. Amendments and updates, including the transition to TRIPS-compliant patent laws and the introduction of Ethical and Regulatory Guidelines, have enhanced India's clinical trial landscape. The Ministry of Health and Family Welfare oversees drug regulation in India through the CDSCO and NPPA. Recent rules, such as the 2019 Medicines and Clinical Trials Rules, aim to streamline and improve clinical trial processes in India. The 2019 rules introduce several key changes, including amendments to the ethics committee constitution, the validity of approved licenses, streamlined application processes, and accelerated approval mechanisms. India's recent regulations align with international standards and aim to improve efficiency and patient safety in clinical trials. The comparison demonstrates the complexity of clinical trial regulations and the efforts made by various countries to ensure the safety and efficacy of new medications while facilitating innovation and drug development. The 2019 New Drugs and Clinical Trials Rules represent a significant shift in India's clinical trial regulations, aiming to simplify processes, enhance patient safety, and maintain ethical standards. Aligned with global norms, these reforms aim to attract investments, foster innovation, and accelerate drug development. Collaboration among stakeholders is vital to address implementation hurdles, strengthen regulatory supervision, and ensure fair healthcare access, positioning India as a leader in clinical research while prioritizing patient welfare and public health.

Sujit Dash   Minaketan Sahoo   Amaresh Chandra Sahoo   Mrityunjay Banerjee   Prabhat Kumar Sahoo   Prabir Kumar Sinha Mahapatra   and Priyanka Muduli   

Among Siddha's internal medicine dosage forms, "Legiyam" stands out as a widely recognized medicinal confectionary. This preparation involves heating decoctions, juices, milk, and sugar to form a syrupy consistency. Drug powders and other ingredients are added, and the mixture is cooled before incorporating butter and honey. "Vaankumaria legiyam," a classic Siddha polyherbal formulation in confectionary form, contains various herbal ingredients known for addressing numerous health concerns, including digestion, diabetes, and skin issues. Commercially available formulations often lack proper standardization, leading to safety and efficacy concerns. In this context, the present study aims to prepare an in-house Siddha formulation using standard raw materials outlined in the Siddha Pharmacopoeia of India. Comparative phytochemical studies were conducted using modern analytical techniques such as AAS, FTIR, HPTLC, and GCMS. The Vaankumari legiyam formulations were tested for heavy metals and trace elements, revealing concentrations below regulatory limits. High-Performance Thin-Layer Chromatography (HPTLC) and Fourier Transform Infrared Spectroscopy (FTIR) analyzed the phytochemical profile, confirming the product's authenticity. Gas Chromatography-Mass Spectrometry (GC-MS) identified and quantified volatile organic compounds, confirming the in-house preparation's reproducibility in capturing aromatic and volatile constituents. These tests confirmed the product's safety for human consumption. The current research has shed light on the potential phytoconstituents responsible for the formulations' claimed therapeutic effects and facilitated quality assessment. The comprehensive analysis of both marketed and in-house formulations of Vaankumari legiyam through various techniques, including phytochemical, physicochemical, AAS, HPTLC, FTIR, and GCMS, has demonstrated consistent equal results.

Nithyapriya V V   Hindustan Abdul Ahad   Harshini Krishnan K V   Ashwin C Kotian   and Prasenjit Prasad   

Microspheres, as versatile carriers for controlled drug delivery, have garnered significant attention in pharmaceutical research because they facilitate drug release kinetics and increase therapeutic efficacy. This abstract presents a comprehensive overview of the preparation of microspheres utilizing factorial design as an optimization strategy. Factorial design, a powerful statistical tool, offers a systematic approach to investigate multiple variables simultaneously, thereby efficiently identifying critical factors influencing the characteristics of microspheres. By systematically varying factors such as polymer type, solvent composition, stirring rate, and drug-to-polymer ratio, factorial design enables the exploration of their individual and interactive effects on microsphere properties. This abstract highlights the key components of factorial design, including the selection of factors and levels, experimental design, data analysis using statistical techniques like analysis of variance (ANOVA), and interpretation of results. Moreover, it elucidates the advantages of factorial design over traditional one-variable-at-a-time methods, such as reduced experimentation time, improved understanding of interactions, and enhanced robustness of the optimization process. Furthermore, this abstract discusses the application of factorial design in optimizing various characteristics of microspheres, containing particle size, morphology, drug entrapment efficiency, and drug discharge profile. By systematically optimizing these parameters, factorial design facilitates the development of microspheres tailored to specific therapeutic requirements, thereby enhancing drug delivery efficacy while minimizing side effects. This abstract underscores the significance of factorial design as a methodical and efficient method for optimizing microspheres in pharmaceutical research.

Bhavana Madupoju   Subhakar Raju Rapaka   Narender Malothu   and Ankarao Areti   

Throughout the past three decades, there has been a notable rise in the incidence and variety of invasive fungal infections due to modifications in medical and surgical care, especially in intensive care units that employ invasive catheters for observing, as well as the use of more potent immune suppression and antibiotic agents. The types, benefits, and limitations of various nanoformulations for the topical and intravenous delivery of antifungal medications are investigated in the current investigation. A couple of instances of NPs used in the delivery of medicines include solid lipid nanoparticles, nanostructured lipid carriers, polymeric NPs, polymeric micelles, phospholipid vesicles (liposomes, deformable liposomes, ethosomes, transferosomes, transethosomes, etc.), non-phospholipid vesicles (noisome and plastics) and dendrimers. Collectively with these features hepatic diseases persist to be a major global health concern and one of the greatest risks to the general population. Even with all of the excellent advances in modern medicine, there are currently no fully effective drugs that improve liver function, provide total organ protection, or promote liver cell regeneration. Therefore, pharmaceutical substitutes for the therapy of liver conditions need to be explored to make them more secure and successful. Focusing liver illnesses may benefit from the use of liposomes, metallic nanoparticles, ceramic nanomaterials, polysaccharides, Carbon-nanotubes, multifunctional NPs, and dendrimers can be made much more effective when these are paired with particular targeted agents.

Duygu Alpaslan   Tuba ErĹźen Dudu   Busra Moran Bozer   Nahit Aktas   and Mustafa Turk   

With the increasing number of cancer cases in recent years, the solution methods suggested for these cases are also of great importance. Within the scope of the presented study, we aimed to develop an alternative material in cancer immunotherapy by synthesizing poly(coconut oil) (p(CnO)) and poly(cacao oil) (p(CcO)) organo-particles from coconut and cocoa oils. The structural features of these particles synthesized using the redox polymerization technique were elucidated by various characterization methods. The chemical structure and functional groups of p(CnO) and p(CcO) organo-particles were determined by Fourier Transform Infrared Spectroscopy (FT-IR). Organo particle size and zeta potential values were determined by the dynamic light scattering (DLS) method using Zetasizer device. The morphological features of the particles were determined by Scanning Electron Microscopy (SEM). Bioactivity properties were determined by antioxidant, antimicrobial and biocompatibility analyses. In this study, the effects of p(CnO) and p(CcO) organo-particles on cytotoxicity and apoptotic processes against L-929 fibroblast and Capan-1 pancreatic cancer cell lines were also investigated. p(CnO) and p(CcO) organo-particles Capan-1 cell lines were determined to have significant cytotoxic activity at all doses studied. An increase in cell number was observed in L-929 fibroblast cells treated with p(CnO) and p(CcO) organo-particles. As a result, findings have been obtained that the p(CcO) organo particle triggers the apoptotic mechanism. On Capan-1 pancreatic cancer cells, p(CcO) was found to have a fatal impact akin to that of doxorubicin. It is anticipated that combining p(CcO) with doxorubicin could potentially lead to better outcomes than using doxorubicin alone.

Achla Vyas   and Kapil Vyas   

The Zebrafish model is more promising and less tedious than other models, so different biomedical research, toxicity studies, genetic research, carcinogenic studies, teratogenic studies, and other behavior studies like anxiolytic, anti-nociceptive, etc. performed on this model. The zebrafish models have demonstrated their efficacy by developing into very effective human disease models, and their use has expanded to encompass several study domains aimed at comprehending the fundamental processes behind the illnesses. Because there is 70% genetic similarity between the zebrafish and human genomes, zebrafish are being used as model animals to better understand the genetics and molecular basis of many diseases. As a result, new and intriguing information about these diseases is emerging, making zebrafish an extremely useful tool for future research. Due to more advantages and fewer complications, increasing numbers of experiments on zebrafish in India, it was required to have CCSEA or any other regulatory guidelines for handling zebrafish. In the year 2021, the CCSEA published guidelines for animal experimentation on fish, in which emphasis was given to the zebrafish model. The present review focuses on different Zebrafish used as research models in various pharmacological activities and CCSEA guidelines for experimentation and handling of zebrafish. Zebrafish are small, easily obtainable, easy to handle, most convenient for administering drug doses, and require a lesser dose overall. Another crucial feature of the transparent embryo of the Zebrafish is its ability to shed light on fish development, neurological development, and other mutation changes that have occurred during research. The majority of the new experimental techniques covered in this article will aid in understanding various approaches and the suitability of the fish model. It will also aid in understanding various factors to be considered when choosing the best model for a given study.

Snigdha Bhardwaj   and Kandasamy Nagarajan   

Candida albicans (C. albicans), the most common and dangerous pathogenic fungus, has been identified as a nosocomial acquired pathogen. Quorum sensing is one method for developing resistance (QS). QS is a cellular mechanism that enables microorganisms to control gene expression in response to changes in cell density through chemical signaling pathways. The pathogenicity of C. albicans is demonstrated by several mechanisms, such as the creation of biofilms, the synthesis of deactivate enzymes, the capacity for phenotypic shifting, and the ability to swiftly transition from the blastophore phase to the hyphal state. Patients who have chronic infections where antibiotics easily take over the host cells but are unable to penetrate the QS mediated biofilms make the antibiotic resistance problem in cases of infections caused by C. albicans more concerning. The anti-virulence agent reduces the pathogenicity without eradicating the target strain, rather than applying abrupt selective pressure to growing microbes. This review presents a current state of scientific research concerning the quorum sensing mechanism in fungi and natural compounds that have been identified as quorum sensing inhibitors and purportedly impede the morphogenic transition of the fungal population. A number of naturally occurring substances, specifically Candida albicans, are emphasized as potentially effective materials with high anti-QS capacities when used as isolated principal components.

Rohini A. Jadhav   Shubhangi J Jadhav   Mahesh R. Gangurde   Vijay R. Gaikwad   Charulata T. Nemade   and Nayana S. Baste   

Natural foods, herbal remedies, and natural healing methods are the best options for a healthy lifestyle. Organic vegetable goods are also in high demand. The use of herbal products has multiplied in the personal care industry. Lips are a pretty organ that can develop conditions including Angular Cheilitis (AC), discolouration, peeling, drying, irritation, and cracking. AC is characterized by the redness and inflammation at the corners of the mouth followed by bacterial infections. So, it needs to be treated with some anti-inflammatory, moisturizing, anti-microbial and antifungal herbal drugs. In the present project, we have designed and evaluated the herbal lip balm effective in Angular cheilitis. The different batches of herbal lip balm were prepared by using the herbs like Moringa oleifera, Lemon grass oil, and neem oil as active ingredients. The excipients like bees wax, paraffin wax, coconut oil and tween 80 were used. The prepared herbal lip balm was evaluated by organoleptic characters, greasiness, pH, melting point, and normal stability study, perfume stability and anti-microbial and antifungal activity. The prepared lip balm has shown good anti-microbial and antifungal activity against the E. coli, P. auriginosa, S. aureus and Candida albican. The best formulation was selected as per the above evaluation. The lemon grass oil, Moringa oleifera leaf extract and Neem oil have shown significant anti-microbial and anti-inflammatory action. Hence, the prepared herbal lip balm can be effective in treatment of Angular cheilitis.

Hital Shah   Hardik Savsani   Kirti Patel   and Tejal Gandhi   

The arachidonic acid (AA) pathway is important in cardiovascular and inflammatory illnesses. Phospholipase A2, a free form of AA, has been metabolized by cytochrome P-450 (CYP450) enzymes, namely the CYP2C (CYP2C6) family (the human analog to CYP2C9), responsible for oxidative stress. This results in the formation of significant mediators: epoxyeicosatrienoic acids (EETs), considered a novel therapeutic target for cardiovascular disease prevention. Fenofibrate,- PPAR-α agonist affects AA metabolism by CYP-450 epoxygenase, resulting in increased synthesis of endogenous EETs having cardioprotective effects. The present investigation sought to determine the effect of fenofibrate on CYP2C6 activity in rats with isoproterenol-induced myocardial infarction. Administration of fenofibrate (100 mg/kg & 150 mg/kg) for four weeks appears to improve mean blood pressure, tachycardia, and cardiac marker enzymes (CK-MB, LDH, and α-HBDH). Fenofibrate dramatically lowered CYP2C6 activity by alleviating oxidative stress through lipid peroxidation (MDA) and restoring natural antioxidant enzymes (SOD, GSH, Catalase). Furthermore, fenofibrate administration restores membrane ATPase activity (Ca⁺⁺ATPase and Na⁺/K⁺ATPase), electrolyte levels (Ca⁺⁺, Na⁺, and K⁺), and prevents ST-segment elevation. Histopathological observations confirm these findings, indicating that the structural architecture of myofibers is preserved and neutrophil infiltration is reduced. According to the current findings, the reduction of CYP2C6 (Human CYP2C9) is an intriguing strategy for the treatment of myocardial infarction and provides novel perspectives for cardiovascular research. In-depth, clinical research is needed to understand the fully effective role of CYP enzymes and their efficacy in the regulation of cardiovascular diseases in individuals.

Mohamed BonewendĂ© Belemlilga   Mathieu Nitiema   Aristide Traore   Eric Nanema   Souleymane Compaore   G. Geoffroy Ouedraogo   Sylvain Ilboudo   Lazare Belemnaba   Noufou Ouedraogo   FĂ©lix B. Kini   and Sylvin Ouedraogo   

Boscia senegalensis is a shrub from semi-arid regions used to treat various pathologies, including inflammation. The aqueous macerate of the leaves was subjected to phytochemical and biological studies to demonstrate its anti-inflammatory properties and safety. The anti-inflammatory carrageenan test and the analgesic acetic acid test were performed. Phytochemical screening of the leaves revealed mainly tannins, flavonoids, sterol glycosides and triterpenes. The LD₅₀ value was 5000 mg/kg. The plant material would, therefore, be classified as having very low toxicity. The evaluation of the anti-edematous activity showed that Boscia senegalensis extract showed the best anti-edematous activity at 1 h with 92.34% ± 0.44 at 500 mg/kg. At the same time, aspegic at 125 mg/kg and betamethasone at 20 mg/kg, used as references, gave 58.51% ± 4.92 and 82.29% ± 2.02, respectively. In the analgesia test, the mean number of contortions was 33 ± 2.64 at 500 mg/kg bw, compared with 30 ± 1.52 for acetaminophen at 100 mg/kg bw. These results justify using the plant in traditional medicine to treat specific pathologies with inflammatory manifestations, such as cough, pain and diarrhoea.

Weiam A. Hussein   Maali D. Alshammari   Weam M. A. Khojali   Nasrin E. Khalifa   Abrar A. Alrashidi   Albndary M. Alenezi   Donia A. Alshelaly   Wejdan.S. Alshehri   Haya A. Albakr   Shahad M. Alshahrani   and Norah A. Alenezi   

In order to facilitate the development of a constituent for traditional medicine, preliminary research pertaining to the detection of secondary metabolites is essential. H. persicum is one of the significant plants in Saudi Arabia, notably in the city of Hail. Analyzing the phytochemical composition of the flavonoid-rich aerial portion of H. persicum with the intention of identifying potentially efficacious medicinal compounds is the principal objective of this study. The extracts contained flavonoids, tannins, alkaloids, and phenolic compounds, as determined by an initial phytochemical analysis. Subsequently, the fraction abundant in flavonoids was identified, and the crude extract's constituents were assessed using the economical, and expeditious thin layer chromatography method. In order to optimize the differentiation of the botanical constituents present in the flavonoid extract, gas chromatography–mass spectrometry was employed. The current investigation additionally aimed to assess the molecular docking and antibacterial activity of the flavonoid-rich fraction of H. persicum, given a shortage of research on this plant. The most potent results were obtained from H. persicum against Pseudomonas aeruginosa and Proteus merabiles.

Janvi Patel   Disha Prajapati   Tanvi Dodiya   and Keshavnam M. Chitte   

Oleanolic acid is a kind of pentacyclic triterpene that is present in a variety of plants, namely fruits and vegetables. Natural plant foods that contain oleanolic acid include apples, ginger, pears, tomatoes, grapes, strawberries, olives, mango, and olive oil, along with culinary and therapeutic herbs, including rosemary, sage, oregano, ginseng, basil, olive leaf, fennel and garlic. Through several in-vitro preclinical investigations, researchers have discovered that oleanolic acid has a wide spectrum of biological properties, including hepatoprotective, anti-inflammatory, anti-diabetes, antimicrobial, antihypertensive, gastroprotective, and antihyperlipidemic effects, as well as cancer treatment. There are several techniques available for the extraction of oleanolic acid from a wide range of species. Extraction from plant species uses various techniques, including soxhlet extraction, sonication, ultrasonic extraction, percolation, cold maceration, and maceration. The major solvents used in extraction are diethyl ether, petroleum ether, n-hexane, ethanol, methanol, ethyl alcohol, and ethyl acetate. Various analytical methods, including HPTLC, HPLC, GC-MS, UHPLC-ESI-MS/MS, UHPLC-PDA, LC-APCI-IT-MS, LC-MS, HPLC-MS/MS, RP-UFLC-DAD, HPLC-PAD-ESI/MS, and others, were employed to identify as well as quantify oleanolic acid in different plant species and formulations. Hence, this review compiles information on the pharmacological actions, extraction methodologies, and analytical methods for investigating and developing methods to assess oleanolic acid from various plant species, herbal remedies, and ayurvedic formulations.

B. Sharannavar   M. Bhagat Amonkar   Apurva Deo   Shailendra Suryawanshi   and Nithyanand Sastry Darbha   

Minoxidil is an anti-hypertensive agent and Tofacitinib citrate is a Janus-kinase inhibitor but there are various articles proving their efficacy in the treatment of Alopecia. An effort is made in order to formulate gel for topical use containing Minoxidil and Tofacitinib citrate for the treatment of Alopecia areata. Objective: The aim of study is to establish and validate a sensitive, selective and precise, method capable of accurately detecting Minoxidil and Tofacitinib citrate in both their raw form and pharmaceutical formulations, adhering strictly to the guidelines outlined by the International Council for Harmonisation (ICH). Method: A UV-spectrophotometric method was devised to simultaneously determine the concentrations of Minoxidil and Tofacitinib citrate. The method underwent validation across various parameters including Linearity, Accuracy, Precision, Repeatability, LOD, LOQ, Robustness, and Ruggedness. A double-beam UV-spectrophotometric technique was developed to simultaneous estimation of the levels of Minoxidil and Tofacitinib citrate. This method was then rigorously validated using various parameters including linearity, accuracy, precision, repeatability, detection limit (LOD), quantification limit (LOQ), robustness, and ruggedness. Results: In the Methanol solvent, Minoxidil exhibits its peak absorbance at 258nm, while Tofacitinib citrate displays its maximum absorbance at 290nm. The concentration range of 2-10µg/mL for both analytes adheres to Beer's law, indicating their reliable quantification potential. For Minoxidil, the Limits of Detection (LOD) and Limits of Quantification (LOQ) stand at 0.537µg/mL and 1.628µg/mL, respectively. Tofacitinib citrate, on the other hand, exhibits LOD and LOQ values of 0.427µg/mL and 1.294µg/mL, respectively. In the assessment of their presence in a topical gel formulation, recovery rates ranging from 50.00% to 150.00% were observed for both Minoxidil and Tofacitinib citrate. Conclusion: The method proposed demonstrates selectivity, specificity, precision, accuracy, ruggedness, and robustness, rendering it suitable for routine analysis of Minoxidil and Tofacitinib citrate in both bulk form and pharmaceutical dosage formulations.

Princy Kashyap   Apurva Yadav   Rajesh Choudhary   Hemlata Sahu   Jaya Shree   and Arvind Kumar Jha   

Cataract is the leading cause of ocular blindness, which mostly occurs in diabetic conditions. In this work, we evaluated the anticataract activity of ethanolic extract of seeds of Abrus precatorius (APEE) against the glucose-induced model in goat lenses (ex-vivo) and the STZ-induced model in albino rats (in-vivo). In the ex-vivo model, goat lenses were incubated in Tyrode solution containing 55 mM glucose for induction of cataract, and APEE (100 and 200 ÎĽg/ml) was assessed against high concentrations of glucose. In the in-vivo STZ-induced model, albino Wistar rats (both sexes, 150-180 g) were treated with a single intraperitoneal injection of streptozotocin (60 mg/kg) for induction of diabetic cataract. After induction of diabetes, STZ-treated rats received APEE (0, 100, or 200 mg/kg/day, p.o.) for the next twelve weeks for assessment of the anticataract activity. Blood glucose level, lens transparency, lens protein contents, and oxidative stress markers were examined for the establishment of anticataract activity. APEE treatments showed potent anticataract activity against both ex-vivo and in-vivo models. When compared to the STZ control group, APEE treatments significantly (P < 0.05) reduced the blood glucose levels, lipid peroxidation (MDA), nitrite content, and insoluble protein contents in lenses and significantly (P < 0.05) increased the antioxidants (CAT, SOD, GPx, and GSH) and soluble protein contents in lenses. We concluded that the ethanolic extract of Abrus precatorius seeds exhibited significant anti-cataract activity against ex-vivo and in-vivo animal models which could be due to its potent antioxidant activity.

Swapna Barhai   Uddip Maity   Sufiyan   and Ayan Sarkar   

This study explores differential pain relief responses to opioids and non-opioids, aiming to establish optimal pain management strategies. The primary goal is to compare the effectiveness of non-opioid and opioid analgesics in managing orthopaedic pain. This prospective study involved 201 participants, spanning in-patient and out-patient settings, with prior and recent orthopaedic diagnoses, including those who underwent orthopaedic surgery. Unwilling, pregnant, or lactating individuals were ethically excluded. Baseline data, including names, ages, and genders, were systematically collected. To investigate pain management strategies, participants were randomly allocated to two groups: one receiving opioid analgesics (tramadol 50 mg or fentanyl 50-100 mcg) and the other non-opioid analgesics (acetaminophen 1 gm/diclofenac 50 mg/ibuprofen 400 mg). Pain scores were assessed using the Wong-Baker scale (1-10) before and after drug administration. Recovery rates, based on pain scores, were used to gauge the relative efficacy of the analgesics. Both groups showed significant pain reduction, with an overall recovery rate of 97.5%. Notably, opioid-treated patients demonstrated favorable recovery rates, while 2.5% of non-opioid patients did not fully recover. Adverse events were more frequent in the opioid group, all of which were manageable. This study suggests that opioid analgesics exhibit superior efficacy in pain management compared to non-opioid analgesics. This research study stands as a valuable asset for clinicians, providing evidence-based recommendations that find a harmonious balance between the robust pain relief provided by opioid analgesics and the appropriateness of non-opioid alternatives for milder cases.

Vidyabhushan Yadav   Hariprasad M.G   Moqbel Ali Moqbel Redhwan   Rahul Kumar   Apurwa Dhavale   and Sourav Guha   

Elevated blood lipid levels, or hyperlipidemia, represents a major modifiable risk factor for cardiovascular pathologies, including atherosclerosis and ischemic heart disease. The exploration of phytochemicals for lipid modulation offers a valuable avenue for therapeutic development. In this context, the present study aimed to elucidate the lipid-lowering potential of ethanol-derived extracts from Moringa concanensis leaves in a controlled experimental setting. Utilizing thirty albino Wistar rats, this research established five distinct groups, encompassing a standard-diet control group and four high-fat diet cohorts to induce a state of hyperlipidemia. Following a month of dietary manipulation, one group continued without intervention, while two groups received varying doses of the Moringa concanensis extract (200 and 400 mg/kg body weight), and another group received a standard hypolipidemic drug, Rosuvastatin, for comparison. After a total of sixty days, systemic and hepatic markers of lipid metabolism, liver function, and oxidative stress were quantitatively assessed. Notably, the Moringa concanensis extract exhibited a dose-responsive amelioration of dyslipidemia, as evidenced by reductions in TC, triglycerides, LDL-C, VLDL-C, and an elevation in HDL levels. Concurrent enhancements in hepatic function and oxidative stress markers—manifested through lowered malondialdehyde levels and augmented superoxide dismutase, glutathione, and catalase activity—were observed. Histopathological examinations corroborated these findings, revealing diminished fat deposition and inflammation within hepatic tissues. Collectively, these results underscore the therapeutic promise of Moringa concanensis leaf extract as a natural agent for managing hyperlipidemia and associated oxidative stress, warranting further investigation for its clinical applicability.

Deependra Soni   Renjil Joshi   Hemkanti Patel   Anshita Gupta   and Chanchal Deep Kaur   

Helicteres isora is a plant with several hidden therapeutic potentials. Due to its possible medicinal benefits, the plant technically called "Indian Screw Tree," Helicteres isora, is frequently used in conventional medical practices. The research presented here seeks to assess the anti-inflammatory and anti-convulsant effects of an extract from Helicteres isora. Rats' paw edema was produced using carrageenan in order to test the anti-inflammatory action. The Helicteres isora extract was given orally in a variety of dosages, and the measurement of paw edema was done periodically. The results indicate a significant reduction in paw edema, highlighting the potential of Helicteres isora extract in alleviating inflammation. In order to evaluate the anti-convulsant activity, mice were induced with convulsions using pentylenetetrazole (PTZ). Various doses of the extract were administered intraperitoneally prior to inducing convulsions. The extract exhibited a dose-dependent decrease in seizure severity and duration, demonstrating its effectiveness as an anti-convulsant. These results support the traditional usage of Helicteres isora in the management of convulsive disorders and inflammatory diseases. It was shown that the extract, when given to rats at dosages of 400 mg/kg, significantly reduced their paw edema after receiving carrageenan over a period of 4 hours. Moreover, when given at a dosage of 400 mg/kg, the extract effectively delayed the onset of convulsions and shortened their duration in the convulsion technique induced by PTZ. These findings suggest that the extract derived from Helicteres isora possesses potent properties in terms of reducing inflammation and preventing convulsions, which can be attributed to its bioactive constituents. To further comprehend the mechanisms behind these effects and identify the specific active substances responsible, additional research is warranted.

Emel Akbaba   

Melatonin is a neuroendocrine hormone that regulates various biological functions. The objective of this work was to conduct a thorough assessment of the molecular targets of melatonin for the treatment of medullary thyroid carcinoma (MTC) via bioinformatics methods. The identification of target proteins for melatonin and MTC was accomplished through the utilization of many databases. A total of 359 gene targets were acquired, then subjected to gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) analyses. The GO subjects indicated a strong association in kinase activity and receptor-ligand activity between the target genes. On the other hand, the KEGG enrichment analysis indicated a significant involvement of the target genes in the PI3K/AKT and MAPK signaling pathways. To identify key genes, an initial step involved the construction of a protein-protein network using the intersecting targets. Subsequently, Cytoscape software unveiled TP53, STAT3, AKT1, JUN, and IL6 as hub genes within the network. The interaction of melatonin and hub genes was validated by molecular docking analysis. The results indicated that melatonin had high binding affinities towards all of the hub genes, with the exception of JUN. The interaction of melatonin and AKT1 had -10.54 kcal/mol binding free energy with several H-bonds and hydrophobic interactions. Also, the melatonin/p53 complex revealed low binding free energy (-9.95 kcal/mol) with strong H-bond interactions. All the outcomes suggest that melatonin induces apoptosis in MTC cells through the PI3K/AKT and MAPK signaling pathways. Therefore, melatonin has the potential to serve as a powerful therapeutic drug for the treatment of MTC.

Sarah Malgwi Gana   Bukar Umaru   Hyellavala Joseph Fomnya   and Patrick Azubuike Onyeyili   

This study aims to determine the effect of oxytetracycline administration on tissue disposition of diminazene aceturate in apparently healthy Sahel goats. Eighteen animals were used for the experiment. Sixteen of the animals were grouped into two with eight animals in each group. The first group was given only diminazene aceturate at 3.5 mg/kg intramuscularly, and the second group received diminazene aceturate (3.5 mg/kg) in combination with 20% oxytetracycline (20 mg/kg) intramuscularly. Diminazene aceturate was administered 30 minutes after the administration of 20% oxytetracycline. Two goats were sacrificed from each group at 5, 10, 15, and 20 days post-administration of the drugs. The two untreated goats were sacrificed to prepare the control tissues and standards. The concentration of diminazene aceturate in various tissues was determined using a chemical assay. Diminazene aceturate administered alone or in combination with oxytetracycline was absorbed and detected in various organs of the treated Sahel goats, with the liver and the kidney recording the highest concentrations. Tissues harvested from goats that received the drug combination presented higher concentrations than the goats treated with diminazene aceturate alone. Drug residues were detected twenty days after drug administration in most tissues of the experimental goats. Diminazene aceturate was found to be present in the tissues of goats for more than 20 days after treatment, hence, 20% oxytetracycline was found to alter the excretion style of diminazene aceturate in goats treated with 20% oxytetracycline.

Rutuja Mali   T. S. Shikalgar   N. S. Naikwade   and Shraddha Parab   

Alzheimer's disease (AD) is a progressive neurodegenerative condition that leads to significant cognitive and behavioural abnormalities, including challenges in learning and memory. Additionally, neuropsychiatric symptoms like anxiety and depression are closely linked to the disease's progression. Consequently, AD gradually erodes various aspects of human life, leading to incapacitation. The underlying causes of AD involve the formation of senile plaques, neurofibrillary tangles, oxidative stress, inflammatory processes, and dysfunction in the cholinergic system. Acetylcholinesterase inhibitors (such as tacrine, rivastigmine, donepezil, and galantamine) are frequently prescribed medications for AD. Nevertheless, these drugs have limitations, including undesirable cholinergic side effects, limited efficacy, potential liver toxicity, and suboptimal bioavailability. As a result, various plant-based compounds have been explored for the treatment of neurodegenerative disorders, including AD. These natural compounds offer the potential for the development of safer, more effective, and multifaceted drugs to address the complexities of AD treatment. The Pithecellobium dulce has many medicinal properties and is widely used in ayurveda. The effect of the extract of aerial parts of Pithecellobium dulce on aluminum chloride induced cognitive dysfunction in zebra fish and mice model was investigated. The primary study was done by using zebrafish model to determine effect of plant extract as they are cheaper and easily available than mice. After that further study was carried out using Mice model to evident the pharmacological activity of plant extract. In Danio rerio (Zebra Fish) and Albino Mice Model, animals were divided into 5 groups, including the Normal, Control (Aluminium chloride), Aluminium Chloride + Donepezil and Aluminium Chloride + P. dulce extract respectively. In Zebra Fish, Spatial memory was evaluated by the colour-biased appetite conditioning T-maze test, while fear memory was measured by the inhibitory avoidance test. In Albino Mice Model, learning and memory were evaluated by Elevated Plus maze test and Morris water maze test. The results suggested that P. dulce extract attenuated cognitive impairment induced by aluminium chloride in zebra fish and Albino Mice Model. Our findings can be useful for further investigation to develop P. dulce extract as an effective health product to treat the Alzheimer Disease.

Mahendra R. Mahajan   Dipak D. Patil   and Ketan B. Patil   

In this work, we devised a practical and efficient RP-HPLC tactic for simultaneously estimating teneligliptin (TEN) and metformin (MET) in both pharmaceutical formulations and bulk substances. Our methodology involved the utilization of a reversed-phase Princeton SPHER-100 C₁₈ column specification (150 Ă— 4.6 mm, 5 ÎĽm particle size) as the stationary phase. Briefly, the mobile phase comprised a blend of 0.025 M potassium dihydrogen phosphate (KH₂PO₄) buffer (pH 4) and methanol in a ratio of 40:60, respectively. The recognition of the compounds was conducted at 249 nm wavelength, with a flow rate maintained at 1 mL/min. The developed approach exhibited excellent proportionality across concentration levels of 25-800 ÎĽg/mL for MET and 5–60 ÎĽg/mL for TEN, with high coefficients of determination (R² = 0.9959 and 0.9958, respectively). Herein, retention times for MET and TEN were determined to be 1.28 and 4.82 minutes, correspondingly. Additionally, recovery rates for MET and TEN ranged from 99.36% to 99.78% and 93.77% to 95.46%, singly. Regarding sensitivity, the limits of detection (LOD) and limits of quantification (LOQ) for TEN were 8.19 µg/mL and 27.30 µg/mL, respectively, while for MET, they were 79.26 µg/mL and 264.20 µg/mL, respectively. The specificity of our tactic was assessed under numerous stress conditions, including exposure to 0.1 M HCl, 0.1 N NaOH, 3% H₂O₂, thermal conditions at 50℃, and UV radiation, demonstrating its robustness.

Harshita Shukla   and Arpna Indurkhya   

In the present study, efforts were made to produce floating beads of glimepiride. The inquiry examined two materials renowned for their straight forward and consistent traits: polymers, namely sodium alginate, and poloxamer 188. Before preparation of floating beads, the polymeric mixture was subjected to foaming stability and foamability. Foamability was found to be in the range of 2.00±0.500 to 14.31±0.422% whereas foam stability was found to be 25.62±1.10 to 86.45±1.72 mins. Nine formulations of glimepiride buoyant beads were prepared, and different methods were employed to scrutinize their attributes, encompassing organoleptic properties, swelling index, buoyancy, drug entrapment, and scanning electron microscopy. Percentage yield was found in a range of 68.56±1.28 to 88.72±2.41. Percentage drug entrapment was found to be in a range of 88.61±2.32 to 96.27±3.16. The in vitro drug release tests revealed that the floating beads exhibited satisfactory results. These tests were conducted in 0.1N HCl solution at pH 1.2, showing a consistent release for up to 12 hours. The SEM images demonstrated the presence of bubbles within the beads, which led to the controlled release of the drug.

Chetan T. Bhat   Panchaxari M. Dandagi   and Pradnya G. Patted   

Aim: This study aimed to develop a safe and effective green solvent-assisted UV-visible spectrophotometric method and validation of an established method for estimating methotrexate in different dosage forms. Method: The solubility profile, melting point, and Fourier Transform Infra-Red were used to characterize the purity of methotrexate (MTX). The drug MTX was analyzed using the UV-visible spectrophotometric method using 1% Sodium Lauryl Sulfate solution in Phosphate buffer saline solution pH 6.8 as a green solvent. The method was validated by using different parameters like linearity, accuracy, precision, specificity, the limit of detection, the limit of quantitation, robustness and ruggedness, and forced degradation studies. The assay of marketed formulation and nano transethosomes was carried out using an established green solvent method. Result: The melting point of pure methotrexate was found 195℃, which nearly corresponds to its actual melting range. FTIR graph by showing sharp characteristic peaks confirmed the purity of the MTX by the presence of functional groups. The wavelength corresponding to the maximum absorbance of the drug was found at 303 nm. The linear range was found with the absorbance of Y = 0.064x + 0.0116 and regression coefficient R₂ = 0.9992 for the concentration range of 2-14 µg/ml of MTX. It was discovered that the repeatability, accuracy, and precision for both intra-day and inter-day were within the acceptable ranges. The limit of detection (LOD) and limit of quantitation (LOQ), which were found to be 0.0825 µg/mL and 0.25 µg/mL, respectively, were determined in order to establish the sensitivity of the technique. Conclusions: The drug MTX was confirmed by the interpretation of UV spectra. This technique may be used for regular analysis of MTX in various pharmaceutical dosage forms and was shown to be easy to use, inexpensive, repeatable, and friendly to the environment.

Albandari Bin-Ammar   

The morbidity of cancer and obesity has been rising at an epidemic rate in recent years. Fatty acid synthase (FAS) is the central enzyme involved in endogenous lipogenesis. It has been postulated that FAS is a viable target for treating cancer and obesity. This study aimed to investigate the FAS inhibitory activity of Euphorbia peplus extract and its secondary metabolites using in vitro and in silico approaches. The inhibitory activity of E. peplus and seven isolated compounds was tested in vitro against chicken FAS due to its similarity to the human enzyme. The results revealed that all compounds as well as the extract inhibited the activity of FAS with compound 2 exhibiting the highest inhibitory activity. The reported IC₅₀ values for the extract were 33.63 ± 0.77 and for 1-7 compounds 38.95 ± 0.98, 19.99 ± 0.35, 22.37 ± 0.62, 27.31 ± 0.95, 24.10 ± 0.47, 22.02 ± 0.63, 66.44 ± 1.59 µg/ml, respectively. In silico work showed the affinity of all compounds toward the thioesterase and KS domains of FAS. All compounds showed hydrogen bonds and hydrophobic interactions with both domains. In conclusion, E. peplus and its secondary metabolites are effective inhibitors of FAS activity and could have beneficial effects against cancer and obesity, pending further investigations.

Jagmohan Padhy   Pradeep Kumar Samal   Rajesh Choudhary   Jaya Shree   and Bharti Vaishnaw   

Numerous studies showed a positive association between depression and obesity. In this context, we evaluated the combined effects of acetyl-L-carnitine and bupropion against high-fat-diet-induced hyperlipidemia model. Experiments were carried out on albino Wistar rats (150-200g, 10-12 weeks of age, both sexes). Experimental animals were housed in various groups containing six animals (n=6) in each group. Further hyperlipidemia was induced by feeding high-fat diets for consecutive 16 weeks. From 13^th week, test groups were treated with acetyl-L-carnitine (100 mg/kg, i.p.), bupropion (20 mg/kg, i.p.), acetyl-L-carnitine (30 mg/kg, i.p.) + bupropion (10 mg/kg, i.p) and acetyl-L-carnitine (50 mg/kg, i.p.) + bupropion (20 mg/kg, i.p.) in respective groups. The percentage of body weight gain, locomotion, blood lipid profile, serum hepatic biomarkers, and oxidative stress markers were examined to assess the beneficial effects of acetyl-L-carnitine and bupropion. The combination of acetyl-L-carnitine and bupropion significantly restored obesity, hyperlipidemia, and oxidative stress conditions, which is indicated by reducing weight gain, improving locomotor activity, blood lipid profile, and hepatic biomarkers, and restoring hepatic antioxidants and lipid peroxidation. Based on the findings, we conclude that the combination of acetyl-L-carnitine and bupropion ameliorates the anti-obesity, antihyperlipidemic, antioxidant, and antidepressant activity and has better effects than individual treatments.

Jelin Vilvest   M. C. John Milton   and Alex Yagoo   

Mosquito-borne diseases pose a serious global health threat, with millions of people affected and a significant number of fatalities each year, underscoring the urgent need for effective control and prevention measures. Conventional mosquito control methods, such as synthetic insecticides, are often ineffective and can have harmful environmental impacts. Therefore, there is a need for the development of new, safe, and effective mosquito control strategies. The objective of this study was to facilitate the advancement of more effective methods for controlling mosquitoes. This study comprehensively assessed the efficacy of successive hexane, chloroform, and methanol extracts derived from Melia azedarach leaves against Aedes aegypti and Culex quinquefasciatus mosquitoes. M. azedarach is a medicinal plant that has been traditionally used to treat a variety of ailments. Successive extracts of M. azedarach leaves were prepared using a Soxhlet apparatus. Evaluations of the extracts' larvicidal, pupicidal, and ovicidal properties against Ae. aegypti and Cx. quinquefasciatus mosquito vectors were conducted. For each extract, lethal concentration 50 (LC₅₀) values were calculated against the two kinds of mosquitoes. The results of this study showed that extracts of methanol and hexane demonstrated notable larvicidal efficacy against Ae. aegypti and Cx. quinquefasciatus mosquitoes, with LC₅₀ values ranging from 113.8 to 135.3 ppm. Additionally, the extract of chloroform showed moderate pupicidal activity as opposed to both types of mosquitoes. However, none of the extracts demonstrated substantial ovicidal activity. The extracts of M. azedarach leaves in methanol and hexane demonstrate potential as potent larvicidal agents against Ae. aegypti and Cx. quinquefasciatus mosquitoes, although the extract in chloroform shows a modest level of pupicidal action. Additional investigation is required to ascertain the active constituents and authenticate these observations under real-world circumstances. These extracts could be used in various mosquito control products, contributing to the fight against diseases like dengue, chikungunya, Japanese encephalitis, and West Nile virus and bolstering global health efforts. The significance of this research is highlighted by their potential involvement in integrated mosquito management programmes, underscoring the need for further research and useful applications to reduce the incidence of mosquito-transmitted diseases.

Keshavnam M. Chitte   Disha Prajapati   Tanvi Dodiya   Janvi Patel   and Rishikesh Wagh   

The present review aims to compile various pharmacological activities, extraction techniques, and analytical techniques for Bergenin. Bergenin, a polyphenol compound that is a C-glycoside of 4-O-methyl gallic acid, has been discovered naturally via several different species, such as Bergenia ciliata, Mallotus Philippines, Bergenia ligulata, Rivea ornata roxb, Bergenia Strachey, Flueggea virosa, Caesalpinia digyna Rottler, Actaea acuminata, Mallotus repandus Muell, etc. Various online search engines like Google Scholar, PUBMED, the National Center for Biotechnology Information, MedlinePlus and Herbal Medicine were used for data mining of published research work. A comprehensive review was compiled, considering the various aspects related to Bergenin. Bergenin exhibits many pharmacological activities, including the ability to stop arrhythmia, HIV, anxiety, fungal infections, viruses, fungal infections, cancer, inflammation, and bacteria. Various methods are available for the extraction of bergenin from various plant species. The profoundly used extraction methods include soxhlet extraction and maceration using methanol as the solvent. The pharmacological actions, investigative methodologies, and extraction methods utilized for identifying and quantifying bergenin and its combinations are covered in detail in the current review. Bergenin can be identified and quantified using various analytical methods such as HPTLC, HPLC, HPLC-MS, LC-MS/MS, LC-MS, UPLC-PDA, and UHPLC-MS. The information compiled in the present review will guide the exploration and selection of analytical methods for evaluating bergenin in plant species, herbal, and ayurvedic formulations.

Srujana Penumuru   Shobha Rani Tenkayala   Gangadhara Ranga   and Ramachandra Bandi   

This study had the objective to establish and validate a reverse-phase high-performance liquid chromatography (RP-HPLC) technique for the quantification of valsartan in its formulations, serving as an indicator of stability. The selected HPLC system employed a UV-07368 column (Instrument ID: QCL-HPL-022), specifically the SHIMADZU LC2010C HT. A novel mobile phase was developed using a volumetric ratio of acetonitrile, water, and glacial acetic acid at 50:50:0.1 (V/V/V), with a flow rate set at 1 ml/min. Detection was carried out at 230 nm. Valsartan underwent stress testing, including UV deterioration, thermal degradation, and hydrolytic degradation in alkaline, acidic, along with neutral circumstances to evaluate the stability-indicating properties of the technique. The method exhibited a linear correlation over a concentration range of 80-240 ppm (r² = 0.999), described by the regression equation y = 21.80x - 188.2. Valsartan demonstrated noteworthy stability under conditions of heat, oxidative stress, acidity, base, and neutrality. The procedure underwent validation for robustness, linearity, specificity, accuracy, and precision. The findings suggested that the method is swift, accurate, precise, reproducible, and dependable, rendering it suitable for analyzing commercial dosage forms in accordance with ICH recommendations.

Sopan N. Nangare   Tejas Dhamane   Divya Patil   Pravin O. Patil   Ketan B. Patil   and Mahendra R. Mahajan   

Diabetes mellitus (DM) remains a persistent and significant global health challenge, profoundly affecting the well-being of individuals. In response to this escalating health concern, the emergence of teneligliptin, an innovative dipeptidyl peptidase-4 (DPP-4) inhibitor medication, presents a promising avenue for managing type 2 DM (T2DM). This comprehensive review aims to provide a thorough examination of the various analytical strategies utilized for the quantification of teneligliptin. It encompasses a range of analytical techniques, including spectroscopic UV analysis, chromatographic approaches such as reversed-phase high-performance liquid chromatography (RP-HPLC), high-performance thin-layer chromatography (HPTLC), liquid chromatography-mass spectrometry (LC-MS), and ultra-performance liquid chromatography (UPLC). Additionally, the focus extends to the detection and quantification of teneligliptin within pharmaceutical formulations. Throughout this comprehensive review, it is noteworthy that the reported lower limit of detection impressively stands at 0.3 ÎĽg/mL, underscoring the remarkable sensitivity of the employed analytical methods. These findings underscore the potential of the developed and validated techniques for accurate quantitative assessment of teneligliptin, both in its pure form and pharmaceutical formulations. In summary, this review represents a significant advancement in the field, shedding light on the available avenues for estimating teneligliptin within pharmaceutical formulations. The analytical approaches discussed herein contribute to the existing body of scientific knowledge and provide invaluable tools for researchers and healthcare professionals dedicated to improving the management of T2DM.

Aarti Tiwari   Kiran Patel   and Pradeep Kumar Samal   

Rheumatoid arthritis, often known as RA, is an autoimmune disorder that has a pathophysiology that is not completely understood. There are a broad variety of elements that may have an effect on its etiology, including environmental factors, genetic factors, microbes, medicines, and hormones. Additionally, it has a substantial influence on the lives of a large number of people. In the majority of instances, DMARDs are the drugs that are used the most often for the treatment and modification of ailments that are associated with rheumatoid arthritis (RA). Nevertheless, there are a great many herbs that might be the subject of study for the modification of diseases associated to rheumatoid arthritis by researchers. We developed our research study in which we generated rheumatoid arthritis (RA) in rats in order to take advantage of the restricted usage of capsaicin in the treatment of rheumatoid arthritis (RA). After that, we investigated the effects of capsaicin on its own and in conjunction with the phosphatidylcholine (PC) complex, and we analyzed the activity of both of these substances. When we compared our findings with those of the illness group, we found that the combination of capsaicin and PC complex had the potential to alter the outcomes that were seen in our experiment. Following the completion of our trials, we arrived to the conclusion that the combination of capsaicin and PC has the potential to play a significant role in the treatment of rheumatoid arthritis (RA).

Cordelia Mano John   Rajamiriyam M   Jonnalagadda Bhavana   Yadav Sangeeta Muthyalaiah   and Sumathy Arockiasamy   

The immunosuppressive agent tacrolimus (TAC), a calcineurin inhibitor (CNI), is a crucial component in solid organ transplantation, contributing to renal damage. CNI-associated nephrotoxicity is majorly manifested in the proximal tubules of the kidney and plays a central role in oxidative stress. As oxidative stress is a contributing factor in nephrotoxicity, the effective antioxidant activity of sinapic acid (SIA; 3,5-dimethoxy-a 4-hydroxycinnamic acid) could help as a novel nephroprotective antioxidant. Studies have shown that polyphenols like SIA exhibit robust antioxidant effects by scavenging ROS, RNS, and mitigating oxidative stress. In this experimental study, the impact of SIA against TAC-induced nephrotoxicity was evaluated in MDCK by measuring cell viability (MTT assay), oxidative stress (ROS), and apoptosis (AO/EB staining). Additionally, levels of lipid peroxidation (LPO), superoxide dismutase (SOD), glutathione (GSH), catalase (CAT), and cell cycle progression were examined. SIA demonstrated the ability to avert TAC-induced cell death and DNA damage. Statistical analysis employing unpaired t-Test revealed a significant reversal of cell cycle arrest, reduced cell population in the sub G₀/G₁ phase, and improved levels of GSH and SOD along with decreased LPO levels with SIA co-treatment. In conclusion, SIA was proved effective in preventing TAC-induced nephrotoxic alterations in MDCK cells.

Archana MR   Seema S Rathore   S. Umadevi   and J. Josephine Leno Jenita   

This study aimed to formulate and optimize the clopidogrel loaded bovine serum albumin nanoparticles as a sustained drug delivery system for effective management of atherosclerosis. The antiplatelet drug clopidogrel has poor water solubility and oral availability of ≤ 50% with rapid first-pass metabolism. The clopidogrel loaded albumin nanoparticles were successfully prepared by the desolvation technique and the Box-Behnken quadratic model which was employed for optimization. For the initial study, the concentration of BSA, 4% v/v glutaraldehyde, and the pH of the polymeric solution were modified and the stirring speed, stirring time, and quantity of drug were kept constant. The process yield, PDI and drug loading were characterized. As the preliminary formulation had higher PDI, particle size and lower drug loading, the formulation was further subjected to optimization by Box-Behnken design. The Box-Behnken quadratic model was employed to optimize the formulation and to study the effect of independent variables like X₁ (Polymer concentration), X₂ (pH), and X₃ (Cross-linking hours) on dependent variables like particle size, PDI, and drug loading. The particle morphologies and zeta potential of optimized CLP-BSA NPs were examined. The efficiency of nanoparticles was confirmed in the Wister albino rats, and the animals treated with CLP-BSA NPs showed prolonged clotting and bleeding time compared to control and clopidogrel drug solution-treated groups.

Neeraj Kumar   Priyanka Sharma   S. C. Joshi   and Utkarsh Kaushik   

Pesticides are the most commonly used substances these days. Pesticides are chemicals that are used to combat toxins that reduce agricultural output. Concerns have been expressed, nevertheless, about its potential negative effects on the ability of both humans and wildlife to reproduce. Pesticides and insecticides are classified into numerous groups. Organophosphates are commonly used pesticides. In order to better understand the mechanisms, exposure pathways, and potential dangers of profenofos and its reproductive toxicity, the goal of this in-depth review is to synthesize the available evidence. Organophosphate insecticides produce a variety of problems in mammals, including physiological, reproductive, and other malformations. The review includes a critical analysis of epidemiological and experimental studies that looked into Profenofos' effects on human and animal reproduction. It draws attention to the possible dangers of exposure to profenofos, including decreased fertility, aberrant development, and poor pregnancy outcomes. In this review, we will focus on Profenofos, which causes reproductive toxicity in the reproductive system of rats, such as decreased testicular size, decreased sperm generation, loss of gametogenesis hormone activity, and effects on the seminiferous tubules, among several others. The article provides a thorough analysis of profenofos and its reproductive toxicity, synthesizing the available research to increase public knowledge of the possible dangers of its use.

Mohammad Ibrahim   Ganesh R Pawar   Shabina Khan   Mohd Mazhar   and Sanchita Pathak   

Despite extensive research outcomes, Alzheimer's disease (AD) still affects millions of people with a high risk of mortality and morbidity around the globe. Currently, over 55 million people worldwide suffer from dementia at present, with 60-70% of cases of Alzheimer's affecting low- and middle-income nations. The majority of AD patients still have insufficient access to feasible treatment choices, so further research is required to find a solution. The usage of herbal medicine is becoming more and more popular due to its natural origins and minimal to nonexistent negative effects when compared to synthetic medications. Therefore, the use of herbal medicines may be an excellent substitute for synthetic medicine for preventing AD. Consequently, we came across to investigate in-vitro acetylcholinesterase and antioxidant potential of Ginkgo biloba as well as revealed its pharmacokinetics, toxicity, and action mechanism by using in silico SwissADME (absorption, distribution, metabolism, and excretion), ProTox-II, molecular docking and network pharmacology. The present observations demonstrated that G. biloba has strong dose-dependent inhibitory potential against AChE (IC50 = 258.31) and DPPH-free radical (IC50 = 124.46). The polyphenols (apigenin and rutin) of G. biloba satisfied the pharmacokinetics/toxicity prediction, which met the five rules of Lipinski's with no violations and did not reveal any toxicity. Furthermore, molecular docking and network pharmacology showed that G. biloba polyphenolic compounds could combat AD by acting on key targets and closely related pathways. In a nutshell, it is quite clear that polyphenols found in G. biloba may replace synthetic medications; however, further large-scale clinical research is required to elucidate the underlying mechanism of action. These studies will encourage further studies that could lead to the development of potential alternative therapies for the management of AD in the future.

Madhavi M N   and Shiva Kumar G   

In the present study, Iguratimod-loaded Cyclodextrin Nanosponges and carboxy methyl tamarind gum interpenetrating polymer networks (IPNs) based tablets were prepared to improve bio-pharmaceutical properties. By varying the concentration of carboxymethyl tamarind gum and glutaraldehyde as cross-linker, Iguratimod-loaded IPNs of formulations (T1-T5) were prepared by freeze-drying, characterized for FTIR, DSC, and XRD and evaluated for % drug loading, equilibrium swelling. Drug-loaded IPN tablets were prepared using Avicel PH-102 and performed in-vitro and in-vivo evaluation studies. The drug load in the IPNs varied between 61.43% and 66.57%, and swelling in the 0.1N HCl presence was significantly less than in the pH 6.8 phosphate buffer. Research employing XRD, DSC, and FTIR confirmed the formation of a molecular complex between Iguratimod and IPNs. The hardness, thickness, mean weight, friability, and average percentage drug content for Iguratimod-loaded IPN tablets were all within limits. Sustain release of drug was observed with IPN tablets in an In-vitro drug release study. In-vivo studies in rabbits estimated various pharmacokinetic constraints AUC_0-�, AUC_0-t, Cmax, Tmax, and MRT. The AUC_0-�, t_1/2, and MRT values of optimized formulations were pointedly more than those with pure drug and commercial tablets. Thus, related to the pure drug and the marketed product, the study's findings showed increased bioavailability and controlled release of Iguratimod from the optimized IPN tablet formulation.

Lavanya Thopireddy   Sathyavelu Reddy Kesireddy   Venkatramana Reddy A.T   and Rajeswara Reddy Saddala   

This study examines the effects of Pimpinella tirupatiensis (Pt) aqueous extract on diabetic rats produced by streptozotocin (STZ), looking at its anti-hyperglycemic, anti-oxidant, and anti-hyperlipidemic activities. Pimpinella tirupatiensis is an indigenous plant of India's Eastern Ghats, namely the Seshachalam mountains. Streptozotocin (40 mg/kg B.W.) was used to cause diabetes in male albino rats by dividing them into five groups of six animals each. The diabetic rats were administered oral doses of 750 mg/kg B.W., per day of Pimpinella tirupatiensis aqueous extract for thirty days. The results showed that the Pimpinella tirupatiensis aqueous extract possessed significantly anti-hyperglycemic, anti-hyperlipidemic, and anti-oxidant activity. Superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GR), and glutathione-s-transferase (GST) activity in the heart tissue of diabetic rats, which was decreased in comparison to normal, were likewise improved by aqueous extract treatment. Additionally, after receiving aqueous extract, the Catalase (CAT) activity, which was markedly elevated in diabetic rats, returned to normal. When diabetic rats were given aqueous extract, the levels of total cholesterol (TC), triglycerides (TGs), HDL cholesterol (HDL-C), LDL cholesterol (LDL-C), and VLDL cholesterol (VLDL-C) in their serum likewise returned to normal. These results imply that Pimpinella tirupatiensis aqueous extract is helpful in managing diabetes by lowering blood glucose levels and preventing oxidative stress by activating cardiac anti-oxidant enzymes.

Dhara Parekh   Vijay Lambole   Vipul Gajera   and Tanvi Desai   

Background: Perilla Frutescens (PF) has traditionally been used in depression-related diseases, as a sedative and anti-oxidant agent. Objective: This study intended to appraise the anxiolytic effects of PF on experimental animals using n-hexane extract (NHE) and ethanolic extract (EE) of PF. Methods: The animals were divided into six separate groups, with each group comprising 6 Swiss albino mice of either sex. PF seeds powder is extracted with NHE, and EE and given orally at a dosage ranging from 1-2 ml/kg of body weight. To evaluate anxiolytic behavior, we employed several tests, including the Elevated Plus Maze (EPM), light-dark exploration test (LDE), open-field test (OFT), Photoactometer (PA), and hole-board test (HBT). Additionally, we assessed various biochemical parameters such as superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH). Result: In the EPM model, both extracts exhibited a significant rise in the percentage of time spent and the number of entries into the open arm. The LDE test demonstrated a prolonged duration of entry into the light box and an increased period spent in the light compartments. Moreover, in the OFT, there was a notable rise in the number of squares crossed. Locomotor activity is measured with a PA, and lower cut-off numbers distinguish extract-treated groups from diazepam-treated normal control groups. The HBT demonstrated a dose-dependent increase in the number of head dips. Conclusion: Both extracts exhibited notable anxiolytic activity, but the most favorable outcome was achieved by administering a 2 ml/kg dose of NHE of PF in all the models. The present research suggests that chemical constituents of PF are an acceptable candidate for the prophylaxis of AD.

Rakesh Mishra   Sagar Dhadwad   Bhawana Sonawane   Chinmay Mali   and Patodi Nidhi   

Quercetin, a remarkable flavonoid known for its extensive pharmacological benefits, faces challenges in its clinical utilization due to issues related to solubility, permeability, and a relatively shorter biological half-life. The study aims to formulate and optimize quercetin nanosuspension to improve bioavailability and to sustain its release. Quercetin nanosuspension is prepared through the precipitation-ultrasonication technique. Gelucire 43/01 and Compritol 888 ATO have been evaluated as lipid polymer stabilizers. The effect of the drug: polymer ratio and probe sonication time were studied and optimized. The optimum formulation of quercetin nanosuspension formulation was also further lyophilized to enhance its stability. The particle size, and entrapment efficiency of prepared batches ranged from 101 ±2.4 to 777 ±1.4nm and 73.65 ±1.61 to 85.89 ±1.56 % respectively. The optimized batch demonstrated a 6-fold improvement in solubility compared to quercetin with 90.45 ±0.84% drug release in 6 h. The results of Ex-vivo absorption studies performed by everted sac technique using rat intestine indicated 87.72+±1.53 % permeation of quercetin from the optimized formulation in 6 h compared to 15.39 ±1.27 % of pure drug. The outcome of the current study indicated that quercetin loaded lyophilized nanosuspension formulation with improved stability could provide a promising approach to enhance its overall bioavailability for its multifarious clinical use.

Suvarna P. Ingale   Anagha M. Joshi   and Pramod L. Ingale   

Alzheimer's disease (AD) is a progressive neurodegenerative, multi-pathological and multifactorial disease affecting around 24 million people worldwide. There are few scientific reports on antioxidant and neuroprotective properties of Passiflora edulis. However, the molecular mechanism of Passiflora edulis leaves in management of AD has remained unexplored. Recently, network Pharmacology has emerged as a newer AI based approach to explore natural product actions and interactions with the multiple targets underlying diseases. Hence, in the present study, we attempted to explore molecular mechanism of Passiflora edulis leaves (PEL) in AD using novel AI based network pharmacology approach. The bioactives present in PEL were extracted from literature sources. Their protein targets were predicted using Swiss Target Prediction web tool. The proteins involved in pathogenesis of AD were retrieved from Therapeutic Target Database. We identified 30 bioactives of PEL modulating 44 potential PEL AD related targets. Of the 30 bioactives of PEL, β-Sitostenone exhibited the highest edge count with interaction with 13 target proteins of AD. Hence, β-Sitostenone has potential to be explored in management of AD. It was found that 44 potential targets of AD were associated with 17 signalling pathways including Alzheimer disease. ADORA2A was identified as the target protein with the highest number of interactions. Further, 14 bioactives have been identified to have AChE modulatory potential which can be explored in management of AD. In conclusion, we identified 27 bioactives of PEL as potential targets which altered majority of target proteins of AD mainly, ADORA2A, ACHE, CHRM3, APP, INSR, BACE1 and MAPT involved in pathogenesis of AD.

Rohit Jaysing Bhor   Nirmal Sujata Eknath   Somnath Suryabhan Gholap   and Santosh Bhausaheb Dighe   

Introduction: Benzimidazole is a heterocyclic hydrocarbon having unique basic structural characteristics in their molecular structure. By treating 5 mL of an organized 20% aqueous extract of Acacia concinna pod in a 250 mL round-bottom flask, a variety of new 1-benzyl-2-phenyl-1H-benzo[d]imidazole (SN1) and its derivatives were created. O-phenylenediamine (1 mmol) was added to the extract above while stirring. After entire addition of o-phenylenediamine, aldehyde (2 mmol) became introduced with continuous stirring at room temperature. Methods: The structure confirmations of synthesized compounds were done by FTIR, NMR spectroscopy and MS. The title compounds and its derivatives were investigated for in vivo anticonvulsant properties by using Wistar Rats. It was done by Strychnine Induced Convulsion Method. Phenytoin is standard drugs for this activity. Structural activity relationship studies reveal that compounds possessing an electron-withdrawing group exhibit better activity than the compounds containing electron-donating groups. Results: Based on the results obtained, when compared to common medicines like Phenytoin, the compounds 4-(1-(4-hydroxy-3-methoxybenzyl)-1H-benzo[d]imidazol-2-yl)-2-methoxyphenol (SN3), 4-(1-(4-hydroxybenzyl)-1H-benzo[d]imidazol-2-yl) phenol (SN4), 1-(4-nitrobenzyl)-2-(4-nitrophenyl)-1H-benzo[d]imidazole (SN5), 1-(2-chlorobenzyl)-2-(2-chlorophenyl)-1H-benzo[d]imidazole (SN6), 1-(3-nitrobenzyl)-2-(3-nitrophenyl)-1H-benzo[d]imidazole (SN7), 1-(4-Hydroxy-3-methoxybenzyl)-2-(4-hydroxy-3-methoxyphenyl)-1H-1, 3-benzimidazole (SN8) give strong anti convulsant effects against phenytoin drug. Conclusion: The title compounds and its derivatives were investigated for anti convulsant Activity. Structural activity relationship studies told that compounds containing benzimidazole derivatives possessing an electron-withdrawing group exhibit better activity than the compounds containing electron-donating groups. The results of the preliminary anti convulsant testing results of the prepared compounds were shown in Table 3. The synthesized compounds were screened for their anti convulsant activity and 1-(4-nitrobenzyl)-2-(4-nitrophenyl)-1H-benzo[d]imidazole (SN5), 1-(2-chlorobenzyl)-2-(2-chlorophenyl)-1H-benzo[d]imidazole (SN6), 1-(3-nitrobenzyl)-2-(3-nitrophenyl)-1H-benzo[d]imidazole (SN7) give strong anti convulsant effects against phenytoin drug.

Vimal Priya Subramanian   Karthika Krishnamoorthy   and Paulsamy Subramaniam   

The species Vincetoxicum subramanii is a traditional medicinal plant of the Apocynaceae family and endemic to Southern Western Ghats, India. It is used to treat ailments such as fever, colds, constipation, diarrhea, ulcers, external tumors, cuts, and relief pain. The present investigation aims to study the phytochemicals, medicinal importance and antioxidant activity of the stem part. The results of the study revealed the presence of total alkaloid content, 70.95±0.60 mg/g in the dried plant material. The ethanol extract of stem has the highest amount of polyphenols - 166.58 mg GAE/g extract, tannins - 99.231 mg GAE/g extract and ascorbic acid - 68,240.7 mg AAE/g extract. However, the chloroform extract was with high amount of flavonoids - 294.04 mg RE/g extract. The highest quantity of saponin - 88.92±1.04 mg DE/g, was noted in hexane extract. The antioxidant assays obtained were highest in stem ethanol extract of the species. The results of this study showed that ethanol extracts from stem of V. subramanii exhibited significant antioxidant activity. Consequently, the results may form the basis for the development of effective antioxidants using V. subramanii, and this would be the first reported scientific rationale to validate its traditional therapeutic use.

Dipanjan Mandal   Lopamudra Saha   Prerona Saha   and Tapan Kumar Chatterjee   

In mammals, biological time plays an essential role in the rhythms of physiology and behavior. Circadian rhythm additionally optimizes the energy balance of the system and metabolic equilibrium. Disruption of biological time will affect this balance and might increase the chance of cardiometabolic disease and type II Diabetes. Obesity and the induction of metabolic disease may alter the temporal order and amplitude of the whole multiple-organ system, enhancing the disease progression. With the development of synergism between the molecular clock and metabolic disease, there is a growing focus and interest in novel clock-related pharmaceuticals and nutraceuticals for treating metabolic dysfunction. This review aims to highlight the importance of biological time within the development of type II diabetes mellitus concerning the clock genes and also the result of mutations of the clock genes that are found to manage glucose homeostasis condition within the system. Thus, this review explored the aspects of biological time and molecular clock that affect illness which might end in the development of Chronotherapy for the treatment of various metabolic diseases and diabetes mellitus.

Karishma Rathi   Ritesh Bhole   Prachi Bansode   and Nayan Motghare   

Alzheimer's disease (AD) is a prevalent and complex neurodegenerative disorder, primarily affecting the elderly population and characterized by cognitive decline. It is primarily diagnosed based on the presence of neurotic plaques and neurofibrillary tangles in the brain. The prevalence of AD is increasing, and existing treatments, such as acetylcholinesterase inhibitors and memantine, aim to alleviate symptoms rather than provide a cure. These treatments have limitations and side effects, leading to the urgent need for innovative therapies. This review discusses the challenges in current AD treatments and explores potential future approaches. Precision medicine, epigenetic interventions, immunotherapy, anti-amyloid and anti-tau agents, and drug repurposing are promising strategies that offer potential benefits in addressing the underlying pathology of AD. Drug repurposing, in particular, is highlighted as a cost-effective and time-saving approach to accelerating drug development. Illustrative examples of repurposed drugs are presented, shedding light on the potential of this strategy to provide effective AD treatments. Moreover, strategies for drug repurposing involve experimental methods like binding assays and phenotypic screening, as well as computational approaches driven by AI. Collaboration among diverse stakeholders and the use of extensive databases enhance repurposing efforts. Examples of repurposed molecules for Alzheimer's disease include anti-diabetic drugs and certain anti-cancer agents, showing potential for AD treatment. Thalidomide's anti-inflammatory properties combat AD-related inflammation. PD-1 blockers like Pembrolizumab activate the immune system against AD. Imatinib shows neuroprotective effects. Antibiotics, antivirals, calcium channel blockers, angiotensin receptor blockers, and erectile dysfunction drugs offer diverse strategies for AD therapy.

Swapnil S. Patil   Manojkumar M. Nitalikar   and Preeti khulbe   

The current study describes a green method to make silver nanoparticles from bixa orellana extract (BOAgNPs). The application of green synthesis for nanoparticle production is considered advantageous in comparison to alternative synthesis methods due to its environmentally friendly nature and cost-effectiveness. Extraction of Bixa orellana seed was carried out by hot extraction technique. The extract was then utilized to prepare silver nanoparticles. The study aimed to investigate the impact of process variables, specifically the concentration of silver nitrate (AgNO₃) and stirring duration, on the particle size and entrapment efficiency of produced BOAgNPs. The ANNOVA of a quadratic model was applied using design expert software to assess the impacts. The optimized BOAgNPs were subjected to characterization using UV and FTIR. The quadratic model provided an optimal batch with a particle size of 88.5 nm and an entrapment efficiency of 95.73%. The observed zeta potential of -35.5 mV indicates that the formulation is likely to exhibit a high level of stability. The analysis of the quadratic model indicates that an increase in string duration results in a significantly increase in particle size. Additionally, an increase in the concentration of AgNO₃ leads to an increase in the entrapment efficiency of BOAgNPs. Nanogel of optimized batch of BOAgNPs has evaluated with In vitro anticancer cell line and it reveals moderate activity against B16F10 cell line.

Idoko A   Firdous S M   Ufedo-Enyo G. Emmanuel   Sofia Khanam   and Ike P O   

This study aimed to scrutinize the effect of the ethanol extracts of leaf and stem bark of Flacourtia indica (F. indica) on blood and liver in aluminum chloride (AlCl₃) challenged Wistar rats. Twenty-four male Wistar rats, weighing 180-210 g were split into six groups (A-F) [n=6], and treated with AlCl₃ (5 days) and extracts (1 week); viz., group A: normal control, group B: AlCl₃ (260 mg/kg), group C: AlCl₃ (260 mg/kg) + leaf extract of F. indica (500 mg/kg), group D: AlCl₃ (260 mg/kg) + leaf extract of F. indica (500 mg/kg), group E: AlCl₃ (260 mg/kg) + bark extract of F. indica (625 mg/kg), and group F: AlCl₃ (260 mg/kg) + bark extract of F. indica (625 mg/kg). In the severe toxicity study, death was recorded at 3500mg/kg bark extract dose. Animals intoxicated with AlCl₃ exhibited a significant rise in the activities of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), blood glucose, and bilirubin (BIL) concentrations; and a decrease in total protein (TP) and albumin (ALB) concentration. Also, a considerable decrease in packed cell volume (PCV) and hemoglobin; and histological artifacts were also remarked in animals intoxicated with AlCl₃. Treatment with the leaf and bark extracts of F. indica exhibited a significant reversal of the above said artifacts. The extracts also improved the histological features of the liver. It may be concluded that treatment of the AlCl₃ induced anemic and hepatic injured rats with leaf and stem bark F. indica, attenuated these conditions effectively, as evident in the reduced concentrations of liver marker enzymes, and improved the levels of PCV and hemoglobin.

Puja Das   Dipanwita Mitra   Dibya Pal   and Debidas Ghosh   

Background: Tinospora cordifolia (Willd.) Miers. traditionally familiar as giloy or gulancha has been used as a traditional folk medicine in Ayurveda from ancient times due to its antifertility effect. However, the mechanisms behind the hypo-testicular action of this herbal plant remain unclear. In this context, this investigation has been performed to unfold the probable mechanism of action by an effective dose of the H₂O-methanol (60:40) extract (HME) of T. cordifolia stem. Objective: To determine the effective dose of T. cordifolia's HME for hypo-testicular efficacy testing in male albino rats. Materials and methods: Doses of T. cordifolia's HME at 5 (low), 10 (moderate), and 20 (high) mg/100 g of body weight (BW)/day for 28 days were given to the experimental rats in three separate dose-treated groups by oral gavage feeding. Rats in the vehicle-treated control group (VTCG) were fed only 0.5 ml sterile water/100 g of BW/day. Spermiological profile, seminal vesicular fructose level, androgenic markers, oxidative stress parameters, and testicular histological studies were analyzed. Results: Different doses of HME-treated groups (HMETGs) delineated a downward deviation significantly (p<0.05) in reproductive organo-somatic indices, spermiological profile, serum testosterone level, androgenic key enzyme’s activities, seminal vesicular fructose level, antioxidant enzyme activity, the diameter of the seminiferous tubules (STD), mitotic and meiotic generations of spermatogenic cell counts at VII^th stage of the spermatokinetics in respect to VTCG. Testicular thiobarbituric acid reactive substances (TBARS) and cholesterol levels were elevated significantly (p<0.05) in the HMETGs in contrast to VTCG. After comparing the HMETGs to VTCG, the changes were noted in toxicity markers at no significant level (p>0.05). Conclusion: The observation enlightens the HME of T. cordifolia stem at the dose of 10 mg (moderate) which executes maximum hypo-testicular activities for male contraception development as well as it also highlighting the therapeutic window of HME in this concern.

Sachin Shivling Bhusari   Akshay Ashok Thorat   and Pravin Shridhar Wakte   

Aim: To develop and validate a simple, precise, accurate, and sensitive UV-visible spectrophotometric method for the simultaneous estimation of Nelfinavir and Quercetin in patented pharmaceutical formulation and bulk by using a first-order derivative spectroscopic method according to the ICH guidelines. Methods: The zero-order spectra were obtained over the range of 200-400 nm for different concentrations of Nelfinavir and Quercetin, the overlay was converted to the first-order derivative spectra and zero-crossing points were selected as working wavelengths. Multiple calibration standards of both drugs were prepared separately and absorbance values were recorded at respective wavelengths. The proposed analytical method was validated according to ICH guidelines and various parameters viz. accuracy, precision, Limit of Detection, Limit of Quantitation, ruggedness, and robustness were assessed. Results: The zero-crossing points of Nelfinavir and Quercetin were found to be 284 nm and 371 nm respectively. The linearity range was found to be between 10-60 ÎĽg/ml for Nelfinavir and 02-10 ÎĽg/ml for Quercetin with a correlation coefficient of 0.999. The intra-and inter-day precision study showed a percent relative standard deviation between 0.44-1.44 and 0.21-1.02 respectively. LOD and LOQ of the proposed method were found to be 0.1195 ÎĽg/ml and 0.3623 ÎĽg/ml for Nelfinavir respectively whereas for Quercetin, said values were 0.0372ÎĽg/ml and 0.1129 ÎĽg/ml respectively. The total percent recovery of Nelfinavir and Quercetin was found to be in the range of 99.86 to 100.02 and 99.71 to 101.57 respectively. Conclusion: The simple, precise, accurate, and sensitive UV-visible spectrophotometric method for the simultaneous estimation of Nelfinavir and Quercetin in patented pharmaceutical formulation and bulk was developed and validated.

Rohit Jaysing Bhor   Somnath Wadghane   Girish Kokate   and Mahesh H Kolhe   

Introduction: 5, 5-diphenylimidazolidine is a heterocyclic hydrocarbon with distinctive basic structural properties in its molecular structure. A novel series of (E)-1-(3-oxo-3-(p-tolyl)prop-1-en-1-yl)-5,5-diphenylimidazolidine-2,4-dione and its derivatives were created by treating different1-acetyl-5,5-diphenylimidazolidine-2,4-dione (0.025 mol) with an equimolar quantity of 4-methyl benzaldehyde. Methods: The structure of synthesised compounds was confirmed using FTIR, NMR spectroscopy, and MS. The agar dilution method was used to test the title compounds and their derivatives for in vitro antibacterial activities against various human pathogenic microorganisms. Ciprofloxacin was used as the standard medication. All of the title compounds were active against some strains of microorganism. According to structural activity connection research, compounds with an electron-withdrawing group have higher activity than compounds with electron-donating groups. Results: Based on the results obtained, when compared to common medicines like Ciprofloxacin; the compounds 4-(2,4-dioxo-5,5-diphenylimidazolidin-1-yl)-4-oxobutanoic acid (SW1)(E)-1-(3-oxo-3-(p-tolyl)prop-1-en-1-yl)-5,5-diphenylimidazolidine-2,4-dione (SW2)(E)-1-(3-oxo-3-(p-tolyl)prop-1-en-1-yl)-5,5-diphenylimidazolidine-2,4-dione (SW3) showed good significant activity. Conclusion: The antibacterial activity of the title compounds and their derivatives was examined. According to structural activity relationship studies, compounds containing 5, 5-diphenylimidazolidine derivatives with an electron-withdrawing group perform better than compounds with electron-donating groups. Table 3 shows the preliminary antimicrobial testing findings of the produced compounds, including the usual broad spectrum antibacterial medication Ciprofloxacin. The synthetic compounds have been evaluated for their capacity to inhibit (E)-1-(3-oxo-3-(p-tolyl)prop-1-en-1-yl) and their antibacterial activity. Derivatives of -5,5-diphenylimidazolidine-2,4-dione (SW2) have significant antibacterial action.

Prashant Gajananrao Karamkar   Ashish Agrawal   and Vivekanand Kisan Chatap   

The present study work was undertaken with the intent to develop a topical emulgel formulation of dapsone 7.5% which would attenuate the first-pass metabolism associated with an oral administration. Dapsone has low solubility and low permeability and is designated as Biopharmaceutical Classification System (BCS) class-II drug as per the biopharmaceutics classification system. The dapsone is formulated as an emulgel which is premeditated to the application by topical route for the management of the skin disease acne vulgaris. The quality target product profile (QTPP) was defined considering product superiority and efficacy. Critical quality attributes (CQAs) are finished product quality metrics and are identified for process validation. The emulgel formulation containing dapsone was optimized by using a 3-factor, 2-level central composed design (CCD). The concentration of polymer, oil, and surfactant were identified as independent variables and drug release and viscosity were dependent variables, Ultrez 10 with a concentration of 1.25 – 4.5 %, Olive Oil with 7.5 – 20 % as oil phase and tween 80 with 12.5 – 37.5 % as surfactant. The optimization study confirms 20 runs which designate a high level of prognostic skill in response surface methodology. The formulations are characterized by drug content, spreadability, pH, residence time, drug release, and viscosity. From the obtained results of drug release, it was concluded that an optimized formulation shows a complete drug release. An accelerated stability study analysis showed acceptable results for an optimized trial formulation.

Anas Dauda   Abba Mus'ab Usman   Albashir Tahir   Ahmad Muslim Muhammad   Suleiman Yunusa   and Aminu Umar Kura   

Inflammation is a common immune response system to obnoxious stimuli like infectious agents, toxic substances injured, cells, or irradiation. However, sustained inflammation can lead to various disease conditions. Therefore, it is important to find ways to counteract or neutralize inflammation. The seeds of Moringa oleifera have been traditionally used for treating several illnesses, but there is a lack of scientific data to evaluate the effectiveness of these practices, thus the aim of this study is to determine whether the methanol extract of Moringa oleifera, obtained through cold maceration, possesses anti-inflammatory activity. The extract effects were assessed using formalin-induced paw edema. Five groups of animals were created, each containing four mice. The groups included a control group (administered normal saline) and a reference group (administered indomethacin). The extract was given at three graded doses; 150, 300, and 600 (mg/kg). Inflammation was induced 30 minutes later by formalin following the extract administration, and measurement of the paw thickness was carried out at 0, 30, 60, and 90 minutes respectively. The results obtained demonstrated a significant reduction in paw thickness at the tested doses. The effect of the extract at 90 minutes was observed to be dose-dependent. This study provides further evidence supporting the traditional medicinal uses of Moringa oleifera seeds.

Lama Alloujami   and Sophie Barguil   

Background: Parabens (PBs) are one of the famous substances used as preservatives for a long time. New studies confirmed that PBs had an estrogen-mimicking effect, which may have an abnormal stimulating effect on cell proliferation and induction of cancer occurrence, particularly breast cancer by their binding of estrogen receptors. As known, estrogen receptors (ERs) are not confined to the breast; they are distributed in many parts of the body including pancreas. The purpose of this research is to investigate the presence of the three types of PBs that are currently used: methyl (MP), ethyl (EP), and propyl parabens (PP) in the samples of pancreatic cancer, which is considered one of the most dangerous cancers. Methods: 12 samples of pancreatic cancer were collected immediately after surgery and kept in -80℃ then PBs had been determined in samples by HPLC/MS. Results: All studied samples had PBs with a total mean (318.8±6.4) ng/g. According to the one sample t-test, clear statistical evidence links the presence of parabens in the studied samples and the incidence of pancreatic cancer. EP was the highest one, followed by MP then PP in samples. Conclusions: Since pancreas have estrogen receptors, and PBs mimic estrogen, and estrogen known by its role in pancreatic cancer, PBs which were detected in pancreas studied samples in very high concentration, may have a role in forming pancreatic cancer tumors by binding with estrogen receptors in pancreas. More studies might be done to understand PBs effecting mechanism in pancreas to determine if BPs may have an important effect in incitation abnormal production of these cells similarly as done in breast cancer cells by binding to ERs in these organs.

Haranath Chinthaginjala   Hindustan Abdul Ahad   Haricharan Kambadur   Naresh Reddy Kamireddy Midde   Rompicharla Narasimha Sai   and Turubilli Satish   

Drug delivery through the skin can be used for efficiently treating local dermatological disorders. Topical gel preparations offer an appropriate drug delivery since they are less oily and easily pull away from the skin. Oral delivery has first-pass impacts, gastrointestinal discomfort, and metabolic degradation as negatives. The topical administration of gel formulations has been suggested as a way to get over these obstacles. The current study is concerned with formulation and In vitro evaluation of C. Papaya topical gel. A tropical plant called Carica Papaya [C. Papaya] has been used for a long time to treat a number of illnesses, including inflammatory conditions. Gastrointestinal issues are the NSAIDs' most significant side effects. In an effort to combat this, a topical gel was created utilizing papaya extract, which is known to cure inflammation. Gels are becoming a top-tier material, as a result of its biocompatibility, network topology, and molecular stability of the included bioactive ingredient, employed for drug delivery formulations. Maceration was the process employed to create the C. Papaya extract, and several polymers, including Carbopol 934, xanthan gum, and guar gum, were used in various proportions to develop the topical gel. The topical gel was prepared by using dispersion method. A total number of six formulations were developed employing 1:1 and 1:5 ratios. It appears that there is no interaction between the extract and the formulation's polymers, according to FT-IR measurements. The topical gel's physical characteristics, viscosity, diffusion studies, pH, and spreadability were assessed and were found to be satisfactory. All of the formulations' viscosities were between 32.3 and 36.4 Cps. Among all formulations, formulation F2 containing 1.5% of Carbopol 934 which shows 98.7% of the drug was released, making it the formulation with the greatest chance of success.

Katike Mohammad Umar   and C. Madhavi Latha   

Drug-related issues affect patients' quality of life, mortality, and morbidity. At any point during the prescription, transcription, distribution, and administration of drugs, drug-related issues might arise. Investigate the prevalence, forms, patterns, and clinical importance of drug-related issues in cardiovascular patients to enhance patient safety and treatment results. An eight-month prospective interventional study was conducted in the medical and cardiology wards of the tertiary care hospital. Drug interactions, untreated indications, and without an indication were the most often reported drug-related problems (DRPs) in inpatients, while subtherapeutic dosage and overdose were the least frequent DRPs. The results of our study indicate that the clinical chemist plays a critical role in the early detection of DRP and the risk factors associated with it, as well as in the assessment and management of any side effects associated with the use of drugs in cardiovascular patients. None of the patients who completed the questionnaire and responded said they experienced any substantial difficulties with their normal day-to-day activities, according to the study. A total of 138 clinical pharmacist interventions were suggested in this research, of which 101 were approved and 37 were refused. Of these issues, 87 were solved, leaving 51 unsolved. According to the study's conclusions, clinical pharmacy is crucial in the early detection of DRP and its associated risk factors to avoid, evaluate, and control unfavourable drug-related outcomes in cardiovascular patients.

Kanwal Asif   Humaira M Khan   Mahreen Siddique   Tanveer Ahmad Khan   Farah Syed   Humayun Riaz   Syed Atif Raza   Abdul Raheem Malik   and Waqas Ahmad   

Stroke is the foremost cause of demise and disability globally. Nevertheless, treatment choices are still inadequate, despite decades of research. The study aimed to assess the neuroprotective effect of Olea europaea (extra virgin olive oil) (EVOE) and Malus domestica (apple cider vinegar) (MD) in the albino rat model of stroke. Their effect on motor and sensory functions (Locomotor asymmetry, forepaw dexterity, contralateral side injury, memory issues, and unilateral deficiency) was measured by cylinder test, pasta test, ladder rung walking test, Morris water maze test, and pole test, respectively. After 21 days of prophylactic dosing, the middle cerebral artery occlusion procedure induced the stroke. After the execution of the animals, 2,3,5 triphenyl tetrazolium chloride (TTC) was used to dye slices of the brain to measure the size of cerebral infarction. EVOE (0.75ml/kg/day) and MD (5ml/kg/day) alone have shown significant neuroprotective potential by improving the findings of the ladder rung walking test (P value < 0.05), pasta test (P value < 0.05), and cylinder test (P value < 0.05) to those fed with the standard dose of Piracetam (250 mg/kg/day). The rats who received EVOE (0.75ml/kg/day) and MD (5ml/kg/day) required less percentage time to reach the hidden maze when compared to rats of the group receiving the standard treatment of Piracetam (P value < 0.05). In the Pole test, mobility duration was significantly reduced by EVOE and MD compared to the treated control group (P value < 0.05). Histopathology showed likewise a significant effect of EVOE and MD on the ischemic part. In conclusion, EVOE and MD have exhibited noteworthy neuroprotective effects.

Abhishek Kumar Pandey   

In India, a wide variety of medicinal plants are reported. Since ancient times, these medicinal plants have been used by people for the treatment of various diseases. The focus of this study is to quantitatively analyze the total phenol, tannin, flavonoid, and alkaloid content, as well as evaluate the in vitro anti-inflammatory activity through HRBC membrane stabilization of the ethanolic extract obtained from Bacopa monnieri [BM]. The plant's antioxidant activity was assessed using the DPPH assay, while its anti-sickling activity was evaluated using the enamel test and the reversibility method. Total phenolic content (TPC) was recorded at 108.76±2.69 µg per mg of gallic acid equivalent. Total tannin content was recorded at 13.49±0.42 µg per mg of gallic acid equivalent. Total flavonoid content was recorded at 191.52±3.90 µg per mg of quercetin equivalent. Bacopa monnieri scavenged 91.24±2.63 % of the DPPH at 75 µg/ml of plant extract. At the same concentrations, the standard drug scavenged 59.14±2.78 % of DPPH. IC₅₀ of plant extract is recorded at 19.23 µg/ml, whereas IC₅₀ of ascorbic acid is recorded at 51.88 µg/ml. The anti-inflammatory activity of plant extract is also dependent on the concentrations. It reduces hemolysis up to 41.5±0.56 % of hemolysis at maximum concentrations, i.e. 2000 µg/ml. At the same concentrations, diclofenac sodium inhibits hemolysis up to 54.55±1.08 %. The reversal rate of the sickle is 81.37±1.25 % with 10mg/ml of Bacopa monnieri extract, while at the same concentrations, standard drug phenylalanine reversed 85.71±1.10 % of sickle cells. The present research shows Bacopa monnieri ethanolic extract has significant anti-oxidant, anti-inflammatory, and anti-sickling activity.

M. Laxmi Kiruthika   E. Shanthi Priya   K. M. Jerun Nisha   D. Sathiya Sheela   and K. Kalimuthu   

Anthropological activities release heavy metals like arsenic, zinc, mercury, lead etc. into the environment and produce pollution disturbing the ecosystem. Chemical synthesis of nanoparticles which is used to curb these effects also emits some toxic substances during the synthesis compared to biologically synthesized nanoparticles. Biologically synthesized nanoparticles also have enormous potential and are used against human and plant pathogens, cancer, inflammation etc. Chemically synthesized nanoparticles (NPs) also contribute to heavy metal accumulation (HMA) while bio-synthesized selenium nanoparticles are known to alleviate the heavy metal accumulation. It is notable that the usage of bio-synthesized NPs in agriculture without knowing the accumulation percentage may lead to HMA. In the present study, the SeNPs are bio-synthesized using the Sansevieria cylindrica plant as a capping and reducing agent. The synthesized nanoparticles are tested on earthworms and termites to eliminate the nanoecotoxicology. The colour change of NP solution ranges from pale yellow to brick red, with an absorption range of SCSeNP as 290~300nm in UV-vis spectroscopy. SCSeNPs showed 6 intense peaks in FT-IR analysis and functional groups such as alcohols, phenols, alkynes, 1°amines, aromatics, aliphatic amines and alkyl halides were identified. 7 intense peaks in XRD such as 20.1°, 23°, 23.92°, 24.24°, 27.96°, 27.96° & 29°, presence of Se in EDAX and size of SCSeNP ranges between 117.2 – 192.2 µm obtained through characterization conform to the synthesis. In HMA study through AAS method, 2.0ppm of accumulation range has been obtained. The mortality rate of earthworms was observed in vitro. This proves that this bio-synthesized SCSeNP can be capable to be used in nano drugs and agriproducts like fertilizer, pesticide and so on.

Shridhar N Deshpande   Elvita Valentine Gonsalves   Akshay Thomas   Aneesh Jeshan Suares   Charan Kumar K. S.   Jesmitha Queeny Dsouza   Mahendra G. S.   and Revanasiddappa B. C.   

Introduction: Thiazolidinediones are widely used synthetic antidiabetic agents. These agents affect the pumping power of heart muscle due to the formation of edema, limiting their usage in patients with congestive heart failure. The current study was aimed to perform in silico docking study of bioactive phytoconstituents from Plumeria acutifolia against the target Peroxisome proliferator-activated gamma (PPAR-Îł). Materials and Methods: The docking study was performed by using Schrodinger. The chemical constituents were retrieved from the PubChem database. The pharmacokinetic and toxicological parameters of each compound were predicted using Pre ADMET online server. The drug-likeness character of each compound was predicted using Molsoft. Results and Discussion: Among the five compounds, two compounds scored positive drug-likeness score. Tremuloidin and Plumieride showed the highest binding affinity with the target protein. All the compounds showed the binding affinity with the target protein suggesting that the compounds from Plumeria acutifolia can be utilized to target PPAR-Îł in the management of diabetes. The study suggests supporting the current study by performing wet lab experiments. Conclusion: The present study reports the presence of some active biomolecules and also presents the probable PPAR-Îł activity via computer simulations.

Gautami S. Penmetsa   Gangolu Meghana   Mohan Kumar P.   NVS Sruthima   Ramesh KSV   and Mohana Kondapally   

Aim and Objective: In spite of its multifaceted qualities, propolis, a herbal remedy that has been used extensively in traditional medicine since the beginning of time, appears to be an interesting addition to topical applications. As an active agent, propolis, when used in various forms such as varnishes, mouthwashes, has been found beneficial in reducing gingivitis, oral mucosal lesions, and oral ulcerations. Therefore, the purpose of the current study is to compare how well commercially available dentifrice and dentifrice containing propolis are at preventing gingivitis. Materials and Methods: For the intervention, two distinct types of paste (Propolis and Colgate) were used on forty participants with mild to moderate gingivitis who were between the ages of 20 and 35. Plaque index (Silness and Loe 1964), gingival index (Loe and Silness 1963), and bleeding scores (Muhlemann and Sons 1971) were recorded at baseline and the 30th day. Results: No statistically significant differences were seen in the intergroup, whereas statistically significant differences (p≤0.05) were observed in the intragroup comparison between baseline and one month. Conclusions: Both the dentifrices were equally effective in reducing clinical parameters.

Thiyagarajan Bharathi   Ganesan Janani   Manokaran Saravanan   and Rajangam Udayakumar   

Raphanus sativus was selected for this study to analyze phytochemicals, IVAD and IVAI activities. The fresh plant of Raphanus sativus was collected and cleaned with pure water. The aerial part and root peel were separated and then dried under shade. The dried plant samples were ground well into powder. About 100 g of dry powder was extracted with solvents ethanol, methanol and benzene by soxhlet apparatus. The extracts were filtered and kept in oven at 40℃ to evaporate the solvent completely from it. Dark brown residues were obtained and kept in air tight containers separately at 4℃ until the time of use. The aerial part and root peel extracts of Raphanus sativus were used for the evaluation of phytochemicals, IVAD and IVAI activities. The phytochemical screening of extracts revealed the presence of phenolic compounds, flavonoids, alkaloids, etc. The ethanolic, methanolic and benzene extracts of aerial part of Raphanus sativus showed IVAD activity as 75.17 ± 3.60%, 71.70 ± 3.47% and 72.61 ± 3.66%, respectively at 250 ÎĽg/ml of concentration. The ethanolic, methanolic and benzene extracts of root peel of Raphanus sativus showed IVAD activity as 78.61 ± 3.62%, 72.73 ± 2.45% and 71.50 ± 3.75%, respectively at 250 ÎĽg/ml of concentration. The IVAI activity was observed in ethanolic, methanolic and benzene extracts of root peel of Raphanus sativus as 83.87 ± 3.55%, 61.82 ± 3.47% and 67.87 ± 3.75%, respectively and the aerial part showed as 82.79 ± 3.65%, 53.97 ± 3.43% and 57.95 ± 3.47%, respectively at 200 ÎĽg/ml of concentration. All the tested extracts were exhibited IVAD and IVAI activities as like as reference drugs acarbose and diclofenac sodium, respectively. So, the results suggest that the aerial part and root peel of Raphanus sativus possess phytocompounds, IVAD and IVAI activities.

Abhishek Kumar Pandey   and Preeti Pandey   

In the present scenario, none of the impactful drugs is available to treat inflammation and oxidative stress without any side effects. We focused on the Ocimum americanum leaf and evaluated its phytochemical composition, anti-inflammatory properties, and antioxidant potential using an ethanolic extraction method. A spectrophotometer was used to measure the leaf extract's overall phenolic content (TPC), whole tannin content (TTC), and the total amount of flavonoid (TFC). The human red blood cell (HRBC) membrane stabilisation method was used to evaluate the extract's anti-inflammatory properties, and the, -diphenyl--picrylhydrazyl (DPPH) method was used to test its antioxidant capacity. We discovered that the TPC, TTC, and TFC values for the plant extract were 131.44 g of GAE/mg, 13.7 g/GAE mg, and 164.7 g of QE/mg, respectively. With a maximal inhibition of 89.79% at a concentration of 1000 g/ml, the extract demonstrated considerable anti-inflammatory efficacy that was comparable to that of the common medicine diclofenac sodium. The extract's capacity to scavenge DPPH was likewise superior to that of the ascorbic acid standard medication, with 96.32% scavenging being seen at the highest concentration (75 g/ml). The extract from the leaf IC₅₀ value was 13.82±2.44 µg/ml, which was one-fourth that of ascorbic acid (51.88±3.24 µg/ml). Our results indicate that the O. americanum leaf extract has the potential to effectively treat inflammation and oxidative stress, and any useful compounds extracted from this plant could be utilized for this purpose in the future.

Anusha B.   Ashwini R.   Sakthikumar C.   Darshan Chhajed D.   Darshan Palavalli   Seema S. Rathore   and J. Josephine Leno Jenita   

L-Carnitine is a non-essential amino acid and is used as an anti-lipidemic agent with bioavailability＜18% when administered orally. A floating system for L-Carnitine was designed to increase the duration it spends in the stomach without coming in contact with the mucosa by solvent evaporation method. 2³ full factorial design model was applied to obtain the experimental runs. The Polymer concentration, stirring rate and stirring time were the constraints of independent variables used to generate the eight experimental runs and were characterized for % yield, in-vitro buoyancy and drug loading. The optimized formulation was studied for its surface morphology, x-ray diffraction, zeta potential and in-vitro release kinetic studies. The formulated microspheres were spherical and free-flowing. They had particle size ranging from 45.75 to 54.79 ÎĽm which was suitable for oral delivery. The % yield ranged from 75 to 87.5% and all the microspheres were floating for more than 24hrs. Ethyl cellulose played an important role as a polymer to achieve the buoyancy and to produce gastric retention of drug. The results suggest that L-carnitine as floating microspheres provides controlled drug delivery for the treatment of hyperlipidemia and also improves the bioavailability.

Ream Nayal   Angela Espir   and Mohammad Y. Abajy   

Obesity is a global issue and can predispose to metabolic diseases such as, type 2 diabetes, atherosclerosis and cardiovascular disease. One of the therapeutic strategies in managing obesity is the inhibition of pancreatic lipase. In this study, the inhibitory activity of different polar extracts of C. azarolus and A. syriacum on porcine pancreatic lipase was evaluated in vitro. Results showed that the best inhibitory activity was for C. azarolus hydroethanolic extract (IC₅₀ =0.204 mg/ml). Therefore, the antiobesity effect of this extract was studied by using wistar rats that had been obese due to a high-fat diet. Oral treatment with 400mg/kg (body weight) of this extract for 6 weeks resulted in body weight reduction similar (p>0.05) to orlistat group (the positive control). Moreover, the ethanol extract decreased significantly the visceral adipose, adiposity index and liver weight in treated group compared to the high-fat control group (p<0.001). Administration of ethanol extract to obese rats on a high-fat diet effectively reduced the elevated plasma levels of total cholesterol and triglycerides (p<0.001). In conclusion, C. azarolus ethanolic extract has good anti-obesity activity and further studies are now being conducted to isolate phytochemicals or fractions that might be used as a novel effective and safe anti-obesity agent.

Richa Sood   Darshitha   Agasa Ramu Mahesh   Seema S. Rathore   and Josephine Leno Jenita   

Nanoparticles of zinc oxide have received huge recognition credits due to unique properties, such as small size, large surface area, optical properties, and morphology. The plant centric approach using several parts and their extracts, is believed to be a recent technique which is simple and an economical strategy in synthesizing metal nanoparticles. This article relates to an easily approachable, environmentally safe and economical technique for synthesizing zinc oxide nanoparticles (ZnO NPs) from the extract of leaves of Centella asiatica. The zinc oxide nanoparticles synthesized were characterized subsequently by Ultraviolet Visible spectroscopy, X-ray diffraction spectroscopy (XRD), Scanning Electron Microscopy (SEM), Energy Dispersive X-ray Analysis (EDX) and Dynamic Light Scattering (DLS) methods. The absorption peak was obtained at 327nm, which indicates formation of ZnO Nanoparticles. The mean particle size and zeta potential were found to be 173.2 and -12.8mV. The X-ray diffraction showed well defined peak characteristic of the nanoparticles. The elemental composition of both Oxygen (O) and Zinc (Zn) was found in the sample with weight percentages 31% and 69% successively; and atomic percentages 64.74% and 35.26%. The surface morphology was estimated by SEM, and it was observed that the particles are almost spherical in shape.

Michael O. Chukwuma   Uchenna E. Odoh   Theodora C. MBA   Vincent O. Chukwube   and Christopher O. Ezugwu   

In 2020, it was estimated that 354 million people in the world live with hepatitis B or C and majority of them lack facilities for testing and/or treatment. Pharmacological activities of some members of the combretacea family have been evaluated and proven. This research aims to investigate Combretum platypterum (Welw.) Hutch & Dalziel leave methanol extract for antioxidant and hepatoprotective activities using paracetamol as toxicant and silymarin as standard compound. Superoxide dismutase, reduced gluthatione, catalase, alkaline phosphatase, aspartate aminotransferase, alanine transaminase and total bilirubin were evaluated as liver function biomarkers. Data was analyzed using SPSS 23 to analyze the data and compare groups, at significance level of p ≤ 0.05. Liver slices were subjected to histopathological examination. 2,2-diphenyl-picrylhydrazyl (DPPH) scavenging, Nitric Oxide scavenging and Ferric Reducing Antioxidant Power, assay methods for in vitro antioxidant activity screening were used. Results of the evaluated parameters showed the group that received only the toxin was different from those that received the toxin and the extract (p < .05). This was corroborated by histopatholical examination. This is an indication that pre-treatment with C. platypterum leaf methanol extract significantly protected the liver. Results of in vitro antioxidant activity evaluation were as follows: DPPH IC50 28.88 ±1.06 μg/ml, AAI=1.34 with ascorbic acid equivalent values of 37.02 µg. The extract had NO Equivalence of 1.0, IC50 = 32.36µg/ml and a FRAP value of 158.67 µM Fe(II)/g dry weight. Combretum platypterum (Welw.) Hutch. & Dalziel. (Combretaceae) possess Hepatoprotective and strong antioxidant properties.

Anitha Puranik   and T. C. Taranath   

The leaf and bark of Erinocarpus nimmonii Grah. ex Dalz., a monotypic, endemic medicinal plant of Malvaceae, were assayed for i) nutritional (proximate, total energy, and minerals) and therapeutic (extractive values, swelling, and foaming index) values using physicochemical parameters, ii) presence of saponin, using Froth Test and Fourier Transform Infrared (FTIR) spectral means, and iii) antimicrobial activity of sequential solvent extracts and minimum inhibitory concentration (MIC) by agar well diffusion and agar dilution methods, respectively. The rich nutritional and mineral value, foaming (saponin), swelling index (mucilage) and maximum soluble extractive values in water and ethanol (SMs) depicted the high nutritional and therapeutic values. Among all sequential extracts, the froth test positively responded to the polar methanol and aqueous extracts, and the FTIR data further validated this finding. The antimicrobial activity showed the highest inhibitory effect of methanol and aqueous extracts towards different clinical isolates like Acinetobacter baumannii and other pathogens, and the bark extracts showed stronger inhibitory effects than the leaf, which may be correlated to the high saponin content of polar extracts and bark, along with other antimicrobial principles. Consequently, the results proved the efficacious therapy for nosocomial infections and ventilator-associated pneumonia-causing A. baumannii (MIC of 0.078 mg/ml). The documented physicochemical parameters assist in maintaining the efficacy and purity of the drug and also recommend its use as a low-cost source of protein and therapeutic drug after further research.

Albashir Tahir   Hauwau Abubakar   Aminu Umar Kura   Suleiman Yunusa   and Yahaya M Katagum   

The use of plants in traditional medicine entails the use of many substances in the cure of both chronic diseases as well as some acute infectious diseases. Herbal medicine is one of the oldest forms of healthcare known to mankind and has been an integral part of healthcare for many centuries, with many people depending on it as their primary form of treatment. Boswellia dalzielii is a plant belonging to the family Burseraceae, which has been widely used in African traditional medicine and was locally reported to have a wide array of medicinal values in folk medicine. The aim of this study is to assess the anticonvulsant potential of the methanolic stem bark extract of Boswellia dalzielii in mice. Phytochemical screening, acute toxicity studies were carried out. The result of the phytochemical screening of the methanol stem bark extract indicated the presence of alkaloids, glycosides, steroids, flavonoids and saponins, and the oral acute toxicity dose was found to be greater than 2000 mg/kg. The extract was tested for anticonvulsant activity against pentylenetetrazole, and strychnine-induced seizures at 100, 200, and 300 mg/kg doses in Swiss albino mice. The extract was observed to significantly (p<0.05) delay the onset of pentylenetetrazole and strychnine-induced convulsions. These results demonstrate that Boswellia dalzielii's methanol stem bark extract has anticonvulsant properties. In conclusion, these findings reinforce the ethnomedical justification for the use of Boswellia dalzielii against convulsions.

Sithara K. Urumbil   Leenitha M.   Jasmin Maria E. J.   and Sherin K. B.   

Gardenia resinifera is a well-known medicinal plant with key contributions in healthcare systems. The qualitative phytochemical analysis of shoot tip exudate of Gardenia resinifera Roth. showed occurrence of bioactive compounds with substantial applications in drug development. Ascertainment of various phytochemical constituents indicated the presence of flavonoids, phenolic compounds, terpenoids, triterpenoids, resins, proteins, amino acids, phlobatannins, phytosterols, quinones, coumarins and gums. Anti-microbial studies using selected pathogenic bacterial and fungal strains showed its ability to prevent microbial growth in agar well diffusion plate. Shoot tip exudate of Gardenia resinifera showed anti-bacterial property against Bacillus subtilis and Staphylococcus aureus. The shoot tip exudate was more effective as anti-bacterial agents than anti-fungal agents. The free radical scavenging activity of shoot tip exudate was analyzed in detail for evaluating the antioxidant potential. Their extracts were analysed using the following assays like 2,2-di-phenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity assay and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonicacid (ABTS) radical cation-based assay which showed percentage inhibition of 93.75±0.52 (1000µg/ml) and 32.62±0.42 (100µg/ml) respectively. The study was based on exudation from shoot tip as a promising source of novel antioxidant without causing any apparent destruction to plant tissues. Plant exudations can be considered as a promising path to be followed for research for the identification of valuable bioresources with great therapeutic value.

Vandana   Ilham Bano   Vinod Deora   and G S Deora   

Tephrosia strigosa of family Fabaceae is an annual herbaceous plant growing in the rocky habitat of the Indian Thar desert. In this study, leaves of T.strigosa were screened for the identification of phytochemical compounds. Preliminary phytochemical screening was carried out on methanolic leaf extract to find out the primary and secondary phytochemical compounds. The secondary metabolites present in methanolic leaf extract were identified by gas chromatography-mass spectroscopy technique. Preliminary phytochemical screening confirmed the presence of primary and secondary metabolites such as carbohydrates, amino acids, phenols, alkaloids, terpenes, flavonoids, phytosterols, glycosides, saponin and fatty acids. GC-MS analysis revealed a total of 55 phytochemical compounds, out of which 52 were identified. Many significant compounds like 2-Methoxy-4-vinyl phenol, Benzofuran, Naphthalene, Neophytadiene, Phytol, Piperidine, Squalene, Lupeol, Hexadecanoic acid and Octadecanoic acid, etc., were reported in methanolic leaf extract. The extract was found rich in terpene compounds. Isolation of various bioactive compounds of T. strigosa can provide an opportunity to develop novel herbal drugs to cure various diseases with fewer side effects.

Lalitha Vivekanandan   Shila Gunasekaran   Sethumathi Ponnusamy   and Prabha Thangavel   

Background: Chronic autoimmune illness rheumatoid arthritis (RA) mostly affects joints and other organs. Free radicals are the main etiology to induce arthritis by increasing the inflammatory mediator's release. The currently available anti-arthritic drugs showed gastrointestinal discomfort, nephrotoxicity, and increased cardiovascular complications due to their long-term use. The herbal drugs have been safe, cheap, and effective against RA. The unripened fruits of Luffa acutangula (LA) or ridged gourd (Family: Cucurbitaceae) are used as an edible vegetable and are reported as a laxative, diuretic, antiseptic, anti-inflammatory, etc. Objective: The present research determined the antiarthritic and antioxidant potential of ethanolic unripened fruit extract of Luffa acultangula (EFLA) against FCA (Complete Freund's Adjuvant) induced arthritic rats. Methods: The subplantar region of rats was treated with single subcutaneous administration of FCA for induction of arthritis. The EFLA at doses of 200, 400 mg/kg/PO, and the Dexamethasone 5 mg/kg/PO were administered from the 16^th to the 30^th day after FCA induction. The total flavonoid and phenolic content were measured by the colorimetric method. Paw edema, arthritic score, hematological parameters, markers for liver and renal function, C-reactive protein (CRP), rheumatoid factor (RF), and markers for oxidative stress were all measured. Results: The total flavonoid content was 0.94±0.02 GAE/g and the total phenolic content was 0.72±0.04 mg of QE/g, respectively. The EFLA significantly attenuated paw swelling, arthritic score, hematological alterations, CRP, RF factor, and free radicals-induced damage. Conclusion: EFLA is a feasible therapeutic drug for the remedy of RA for long-term use because it is an antioxidant-rich edible fruit. Further research is needed to find prophylactic actions and adjuvant therapy of LA against RA.

Burak Yaman   

In this research, it is aimed to determine the potentiation of pindolol on the antidepressant effect of venlafaxine in psychomotor agitated depressed mice exposed to chronic mild stress by using open field test and measurement of defecation score. Psychomotor agitated depression model was created by a modified chronic mild stress protocol inspired by previous studies where chronic mild stress was used to provide a depression model in mice. Antidepressant effects of the drugs were tested by measurement of transition to the center area, time in the center area and defecation score of mice in open field test. Chronic mild stress caused to increase in the transition frequency to the center area, in the time to be in the center area, and in the defecation score, markers of the psychomotor agitation and depression (p<0.05). Venlafaxine-pindolol combination but not venlafaxine or pindolol only reversed this effect (p<0.05). Pindolol increased the antidepressant effect of venlafaxine and venlafaxine-pindolol combination had been enough to reverse psychomotor agitation triggered by chronic mild stress, while venlafaxine alone was not enough in the same dose. Chronic mild stress administration resulted in a significant increase in the defecation score of animals (p<0.05). Venlafaxine-pindolol combination reversed the defecation score to control levels but not venlafaxine or pindolol alone. In this study, psychomotor agitation symptom of depression was created with a modified chronic mild stress model applied for the first time in Balb/c mice. Pindolol has the potential to potentiate the venlafaxine in psychomotor agitated mice exposed to chronic mild stress.

Sakshi Bhardwaj   Dhanashree Javere   Pradnya Bagad   Likhit Akotkar   Vivekanad Chatap   and Urmila Aswar   

Black rice (Oryza sativa L. indica) is also called purple rice (gluten free rice), emperor's rice (tribute food) and king's rice. It is abundantly grown worldwide, specifically in Asian countries such as Bangladesh, China, Japan, Sri Lanka, Indonesia, and Thailand. In India, it is majorly found in north-eastern states, including Meghalaya, Assam, and Manipur, which are the cultivators of black rice. It is also considered a superfood owing to its potent antioxidant activity which mediates numerous health-beneficial effects with anticancer, anti-inflammatory, immunomodulatory and anti-allergic characteristics. Black rice has a high nutritional value due to its rich source of various vitamins (A, B, E), amino acids and lipids, dietary fibre. The presence of the flavonoid plant pigment anthocyanin contributes to its purple-black colour and strong antioxidant properties. Other components like manganese and calcium support a healthy metabolism and stronger bones. Black rice is getting popularized in recent times because of its very low toxicity and higher nutritional qualities. This review focuses on the nutritional composition, toxicity, pharmacological uses and future opportunities of black rice for better health and well-being.

Prashant B Patil   Darshan D. Mahale   Bhushan K. Marathe   Kiran P. Sinkar   Dilip A. Patil   Jayvadan K. Patel   and Zamir G. Khan   

Recently gelatin nanoparticles (G-NPs) have been gaining substantial consideration because they offer excellent properties like low cost, biocompatibility, and biodegradability. One of the protein materials that can be utilized to make nanoparticles is gelatin. The emphasis is constructed on the datum that gelatin is non-toxic, easy to crosslink, and chemically changeable, and hence consumes a gigantic potential for colloidal drug delivery system synthesis. The surface of G-NPs can be easily cat-ionized with a variety of amine derivatives to provide targeted and sustained drug delivery. Curcumin-loaded gelatin G-NPs were manufactured using a two-step desolvation progression in this study. A glutaraldehyde cross-linker was also employed to provide G-NP with good stability. Inclusive, the ordinary size of the curcumin-loaded gelatin (CGNPs) was 112 nm, with a zeta potential of +31.80 mV. An In-vitro dissolution study confirmed 88 % of the drug was released from the CGNP within 24 h. In comparison, drug release showed a lower release rate, at about 66 % after 24 h. In the present work, we fabricated a curcumin-loaded gelatin nanoparticle to improve the solubility and thereby enhance the stability of a formulation, which will further encourage the progress of curcumin based on nanoformulation. Curcumin-loaded gelatin nanoparticles have a higher stability in biological fluids than colloidal carriers, allowing for the desired delimited and unrelenting release of encapsulated drug molecules. In all, the fabricated curcumin-loaded gelatin nanoparticle proved to be a sustained-release drug delivery system.

Arun Kumar Kashyap   Padmini Bisoyi   and Buddhi Prakash Jain   

Macrotyloma uniflorum (Horse gram), a legume plant with medicinal properties is used as a tonic, diuretic and in the treatment of rheumatism and neurological disorders. The present study was undertaken to find the anti-microbial, anti-inflammatory, the antioxidant, and cytotoxic activity of leaf extract of Macrotyloma uniflorum. Extract of the Macrotyloma uniflorum leaf was prepared in the hexane, ethyl acetate, methanol solvent and analyzed for phytochemicals composition. Total flavonoid and phenolic contents, antioxidants, and free radical scavenging capacity were determined and found to be high in methanolic and ethyl acetate extract compared to the Hexane extract. The methanolic extract showed higher anti-microbial activity and anti-inflammatory activity. Methanolic extract of Macrotyloma uniflorum leaf has the anti-microbial, antioxidant, and anti-inflammatory properties. The leaf extract of the Macrotyloma uniflorum also shows cytotoxic effects in breast cancer cell line (MCF-7) in a dose dependent manner which was further confirmed by FACS analysis. This study highlights the potential of the methanolic extract of leaves of Macrotyloma uniflorum -as an antioxidant, anti-inflammatory, cytotoxic and anti-microbial agent.

Sandip Badadhe   Gurdeeep Singh   and Neetesh Jain   

The Gamma Oryzanol (GOZ), the concept of biopharmaceutical classification systems (BCS), methods for enhancement of solubility and bioavailability, gamma oryzanol have been used for a number of applications, especially due to strong antioxidant activity and lipid-lowering properties. As gamma oryzanol has many therapeutic effects, it can be beneficial for the pharmaceutical industry. But the use of gamma oryzanol in clinical and functional meals systems may be restrained due to low water solubility, poor bioavailability and fast metabolism of gamma oryzanol. -Oryzanol is insoluble in water. Numerous methods of solubilizing complex for cosmetic, pharmaceutical, food uses have been defined. Based totally on initial showing of changed dropped SNEDDS formula, eight components of GOZ stacked SNEEDS have been organized utilizing Capryol 90, Labrasol and Transcutol HP as oil, surfactant as well as cosurfactant, separately. Some of the extraordinary surfactants screened, Labrasol confirmed exceptional solubilizing capability for GOZ (94.69±1.04 mg/mL). On one hundred fold dilution, the percentage transmittance of GOZ SNEDDS formula was observed to be among 97.87% ± 0.30% and 99.57% ± 0.06%. From droplet size analysis, it was seen that GOZ loaded SNEDDS formulation had the mean particle size in the range of 15.03±0.18 to 22.97±0.44 nm indicating their efficiency as SNEDDS. Visual perception showed that there was no stage partition or any flocculation in all formulations and the actual appearance of all plans in underlying one hour of in vitro discharge research, just 12.23% ± 0.45% as well as 42.33% ± 2.78% of GOZ was dissolved after pure drug as well as advertised tablets correspondingly.

Abhishek Kumar Pandey   and Preeti Pande   

Aegle marmelos is a deciduous tree with trifoliate leave commonly found in the Indian subcontinent. The present study is to diagnose the phytochemicals physiochemical, qualitative and quantitative estimation. Total phenolic content was recorded at 53.52±3.25 µg Gallic acid equivalent (GAE) /mg of plant extract, total tannin content was observed at 6.4±1.02 ÎĽg GAE/mg and total flavonoid content was recorded at 37.4±2.65 ÎĽg Quercetin equivalent/mg. The study also comprised the Anti-inflammatory and anti-oxidant activity of plant leaves. Anti-inflammatory activity was examined through the HRBC method and compared with the standard drug diclofenac sodium. Ethanolic extract of leaves shows significant anti-inflammatory activity and provides 61.04±2.89 % of protection against hemolysis at 2000µg/ml of leave extract whereas at the same concentration diclofenac sodium provides only 54.55±2.35 % protection against hemolysis. The antioxidant potential of plant extract examines through DPPH free radical scavenging method. Leave extract showed better antioxidant activity in comparison to ascorbic acid. IC₅₀ of plant extract is 48.99 ±1.96 % which is also better than the value of IC₅₀ of ascorbic acid which was recorded at 50.39±2.05. The study showed that leaves extract of the plant has significant potential for the treatment of oxidative stress and inflammation.

K. Bhuvaneswari   KM Jerun Nisha   K. Kalimuthu   M. Lakxmi Kiruthika   E. Shanthi Priya   and Sathiya Sheela D.   

Introduction: The present study focuses on the use of Leucas aspera aqueous extract as a reduction agent for the synthesis of copper nanoparticles (CuNPs). The entire plant is employed in conventional medicine and as an insecticide. Scientific research has been done on the plant's potential as an anti-inflammatory, analgesic, and wound-healing agent. Intoxication by cobra venom also makes use of it. This study was intended to explore the in vitro anti-inflammatory, antidiabetic and anticancer activities of copper nanoparticles. Methods: Protein denaturation and membrane stabilization of human red blood cells (HRBC) were used to assess the in vitro anti-inflammatory activity. The antidiabetic activity of the CuNPs was evaluated by inhibiting both amylase and glucosidase in vitro, whereas anticancer activity against vero and MCF-7 cell line. Results: The Leucas aspera copper nanoparticles (LACuNPs) showed a dose dependent -inflammatory activity. The highest inhibition percentage in protein denaturation is 70.30±1.72% and 67.68±1.41% in HRBC membrane stabilization at 1000µg/ml concentration. In vitro antidiabetic activity exhibited 76.03 ± 1.14 of α-amylase and 71.54 ± 1.55 at α-glucosidase inhibition assay. The in vitro anti-cancer study revealed 50% apoptosis (IC₅₀) of LACuNPs treated vero and MCF7 are displayed as 248.84±0.01 µg/ml and 137.39±1.51, respectively. Conclusion: The results clearly demonstrated the application of biosynthesized LACuNPs as potential anti-inflammatory, anti-diabetic, and anticancer agents in addition to their environmental friendliness.

Abdullah A. A. Alghamdi   Nada M. Ali   Mohammad Mahboob Alam   Syed Nazreen   and Ali Mahzari   

Antioxidants, in addition to protection against oxidative stress, also possess anti-inflammatory and anticancer potentials. In this work, the ethanolic extract (EE) of Euphorbia inarticulata has been evaluated for antioxidant, anti-inflammatory and anticancer activities. The antioxidant activity showed that EE significantly scavenges DPPH (IC₅₀ = 54.56 ± 2.38 µg/ml) and H₂O₂(77.44 ± 2.76 µg/ml), whereas ferric reducing antioxidant power (FRAP) and total antioxidant capacity (TAC) were found to be 100.93 ± 4.15 µg/ml and 46.72 ± 3.86 mg gallic acid equi/gm, respectively. The EE exhibited significant inhibition on COX-1 (IC₅₀ 79.84µg/ml) and protein denaturation (IC₅₀57.6 µg/ml), compared to indomethacin and diclofenac, respectively. Furthermore, EE was found to be effective in killing Huh-7 and HeLa cancerous cells with IC₅₀ 104.62 (SI 2.36) and 145.11 µg/ml (SI 1.7), respectively, while doxorubicin displayed IC₅₀ 0.71 (Huh-7) and 2.63 µg/ml (HeLa), whereas it was safe on normal MRC-5 cells. The HPLC analysis showed the presence of ellagic acid, caffeic acid, gallic acid, syringic acid, cinnamic acid and catechol which may be responsible for the promising antioxidant, anti-inflammatory and anticancer potentials exerted by the ethanolic extract of E. inarticulata. These results conclude that Euphorbia inarticulata ethanolic extract has anti-inflammatory and anticancer effects by triggering oxidative stress.

Imran Uysal   OÄźuzhan Koçer   Falah Saleh Mohammed   Ă–mer Lekesiz   Mehmet DoÄźan   Ali Erdem Ĺžabik   Emre Sevindik   Filiz Ă–zbas Gerçeker   and Mustafa Sevindik   

Complementary medicine has emerged with the history of humanity and has become widespread with the use of natural products in the treatment of many diseases. People have used many plant species in the treatment of diseases by benefiting from trial and error and knowledge. Plants have been used as shelter, food, medicine, spices, cosmetics, and tools for use in religious rituals. Different communities around the world have widely used local plants. In addition, the cosmopolitan species are used by all people in the treatment of diseases. Genus Salvia is a plant species that is widely known and used worldwide for its nutritional properties as well as its many biological activities. There are many secondary metabolites in different parts of the plant. Thanks to these secondary metabolites, it shows different biological properties. Salvia species have remarkable activities such as antioxidant, antimicrobial, anticancer. It is also an important natural resource with its high nutritional content. In this study, the nutritional contents, usage areas, chemical compositions and pharmacological properties of Genus Salvia were reviewed. In this context, the use of Salvia species in pharmacological designs and their nutritional importance were emphasized. As a result, it has been determined that members of Genus Salvia are one of the important plant species used in complementary medicine.

Jyotsana Suyal   Bhavna Kumar   and Vikas Jakhmola   

The self-nanoemulsifying drug delivery system is solitarily the most frequent dosage form for administering drug molecules towards the target region in the pharmaceutical industry. It has gotten a lot of interest in the current scenario because of its budding applications in various industries. In the pharmaceutical business, self-nanoemulsifying drug delivery systems have been used to distribute medications via oral, topical, and parenteral routes. SNEDDS are submicron-sized emulsions being researched as drug carriers to improve therapeutic agent delivery. Due to their tiny droplets, elevated solubility ability, broad interfacial region, reduced consistency, transparent or semi-transparent emergence, & remarkable kinetic constancy, self-nanoemulsifying medicines are meant for an extensive choice of application. Through a combination of a water-insoluble lipid phase with a high-stress aqueous phase, these emulsions may be manufactured in huge quantities quickly. These are created using surfactants, co-surfactants, and co-solvents. In BCS class II and IV drugs, the self-nanoemulsifying drug delivery system is useful in favor of increasing the water solubility of water-soluble pharmaceuticals. In this review, various aspects of the self-nanoemulsifying drug delivery system are highlighted, including method of preparation, characterization techniques such as particle size, zeta potential, polydispersity, drug content, advantages, disadvantages, and a particular importance on various applications of SNEDDS in different areas, such as cancer treatment, drug targeting, and as a vehicle for transdermal drug delivery.

Shivraj Popat Jadhav   Santosh Kumar Singh   and Himmat Singh Chawra   

The formulation development of a drug is majorly based on the solubility of drugs. Nearly 40% of newly developed drugs show poor water solubility. Several approaches are used for the increasing solubility of such drugs for formulation development. Nanosuspension is one such attractive tactic which can be used for the enhancement of solubility, stability as well as bioavailability of such drugs. Nanosuspension can be defined as a two-phasic dosage form where solid drug particles of size less than 1 ÎĽm are dispersed in an aqueous phase with the help of a stabilizer. Particle size reduction in the nanoscale causes an increase in the surface area leading to an increase in dissolution rate and ultimately bioavailability is increased. A variety of excipients are used for the formulation of nanosuspension. Stabilizers, surfactants, co-surfactants, natural as well as organic solvents, buffers, salts, polyols, osmogents, and cryoprotectants are used in the formulation of nanosuspension. Various methods used in the formulation of nanosuspension can be classified into top-down and bottom-up approaches. Wet milling, high-pressure homogenization, anti-solvent techniques, melt emulsification, supercritical fluid extraction and ultrasonic homogenization are some of the methods for the preparation of nanosuspension. These methods are easy and appropriate for all poor water-soluble drugs. Nanosuspensions technology can be applied for the preparation of oral, pulmonary, injectable, ocular as well as targeted drug delivery. This review emphasizes various advantages and disadvantages of nanosuspension, its methods of preparation, formulation approaches, evaluation parameters, pharmaceutical applications, marketed products and patents of nanosuspension.

Hajra Parveen   Vanitha Kondi   and Ramesh Alluri   

The goal of the research was to formulate floating microsponges of Olmesartan medoxomil by 3² factorial design to enhance bioavailability in the gastric region. The quasi-emulsion solvent diffusion method was used to prepare gastroretentive floating microsponges. In this study, the concentration of Eudragit L-100 (X₁) and the concentration of polyvinyl alcohol (PVA) (X₂) were chosen as independent factors at three distinct levels using Design-Expert® software (trial version 13.1.0, Stat-Ease). The dependent variables chosen were the % Buoyancy (Y₁) and % cumulative drug release (Y₂). The percent yield, particle size, bulk density, % buoyancy, % entrapment efficiency, in vitro drug release, the kinetics of drug release, variation of the model, Fourier Transform Infrared Spectroscopy (FTIR) studies, and stability studies for the optimized formulation were conducted. From the design expert, the optimized formula was found to be OLM-MSG7. The magnitude of the coefficient of both X₁ and X₂ showed a positive effect on the buoyancy of the floating microsponges. As the concentration of eudragit L-100, the buoyancy of the microsponges increased. The reason for the buoyancy due to the high concentration of eudragit L-100 may be attributed to the low density of the polymer. However, an antagonistic linear effect of PVA was observed. X₁ and X₂ i.e., polymer concentration and PVA had a positive effect on % CDR of microsponges which indicates that the higher amount of eudragit L-100 contributes to an increase in % CDR. FTIR studies show there is no chemical interaction between the drug and the polymer in the formulation.

Prashant Gajananrao Karamkar   Ashish Agrawal   and Vivekanand Kisan Chatap   

Application of drug by topical route is an alternate route for the treatment of skin diseases for systemic route. The skin diseases can be treated by administration of drug by local application and may avoid first pass metabolism. It minimizes systemic side effects and when applied locally can be removed easily if any side effects occur like, irritation, skin rash, redness at the application site. The topical drug delivery has been beneficial for longer period of time because of availability of large surface area of skin which exposed to circulatory routes. Because of this route, one can be directly applied to any external body surface and it is only for local application. Amongst many types of topical dosage form delivery, gel is most likely to be used and is a patient-friendly dosage form. Due to the lack of insoluble excipients and oily bases, the gel represents better release of drug as compared to other topical drug delivery system. Nowadays, many industries follow QbD (Quality by Design) approach for the formulation of Gel to prepare a quality medicine delivery to patients. The QbD approach describes the CQA, CMA and CPP of the formulation which ensures the quality of dosage form. This review article focuses on the different dosage forms, types of gel, evaluation by taking parameters such as drug content, pH, spreadability, extrudability, viscosity, swelling index and in-vitro drug diffusion and application of QbD approach to gel formulation.

Nur Faeqah Furairah Othman   Gurmeet Kaur Surindar Singh   and Nurul Aqmar Mohamad Nor Hazalin   

Dementia has become one of the most significant public health and economic burdens. Due to the absence of a cure for dementia, the public health priority has focused more recently on the intervention that may help to improve cognitive performance in older age or at least delay the onset of dementia. Recently, nutraceuticals have displayed the ability and strong potential to act as neuroprotectants and/or delay cognitive impairment through various neuroprotective mechanisms. The present study aimed to review scientifically the potential of nutraceuticals in preventing and/or restoring cognitive function and highlights their possible mechanisms and evidence mainly through the modulation of neurotransmitters. Online literature databases such as PubMed and Science Direct were used to search related articles. Current evidence revealed that nutraceuticals like choline, iron, galantamine, omega-3, luteolin, theanine, some vitamins, and probiotics showed better neuroprotective activity against cognitive impairment and dementia. The neuroprotective activity of these nutraceuticals is associated with their ability in regulating neurotransmitters, including inhibiting the reuptake enzymes of neurotransmitters, up-regulating the receptor level, and becoming the precursors of neurotransmitters, thus enabling neurotransmission to occur. Hence, this review would aid the researcher and common people in better understanding the mechanisms and choosing better nutraceuticals to combat cognitive decline and dementia.

Rohit Jaysing Bhor   Komal Sakharam Sable   Mayur Shivaji Bhosale   and Santosh Bhausaheb Dighe   

Introduction: Benzimidazole is a heterocyclic hydrocarbon having unique basic structural characteristics in their structure. This moiety was formed by using aromatic benzene and imidazole heterocylic ring. This molecule gives great application in biological and clinical studies. Benzimidazole and its derivatives have versatile Nitrogen containing heterocyclic compounds that give a promising category of biologically active compounds and possess a wide selection of biological activities like antibacterial drug, medicament, anti-ulcer, anti-diabetic, etc. Objective: Several scientists have declared that benzimidazole system possesses the variable sites like the position of a pair and five which might be fittingly changed to yield potent therapeutic agents. The current review covers the chemistry and medicine activities of substituted benzimidazoles. Materials & Methods: Formic acid; Acetyl Chloride; Hydrazine; Benzene-1,2-diol; Glycolic Acid; Benzoyl Chloride; Methyl Chloride; Ethyl Chloride; Benzamide etc. and methods are TLC, IR spectra, ¹H-NMR and MS. Results & Conclusion: The pharmacological screening was done by using PTZ Induced Convulsion Method for anticonvulsant activity. The synthesize compounds were established to be BA to BK. The compound BA, BC, BJ, BI and BK were established to be the most potent compound through the comparison with standard drugs phenytoin. Synthesized newer benzimidazole derivatives were screened for Anti-convulsant activity. It was seen that in biological activity, derivatives containing 2-nitro aniline and 3-nitro aniline have more significant biological activities than other benzimidazole derivatives. Total 11 compounds (4 Step Products + 7 Benzimidazole Derivatives) were evaluated for their biological screening.

Jahasultana Mohammed   Prasanna Kumar Desu   J. Risy Namratha   and GSN Koteswara Rao   

The star of the carbon nanomaterials industry is now carbon dots (C-Dots). C-Dots are a potential tool because of their applications in imaging, environmental, catalytic, biological, and energy fields thanks to their numerous distinctive physicochemical and photochemical characteristics. C-Dots have received plenty of research attention and have shown remarkable application growth to date. Green biomass or sustainable raw materials may be used to create C-Dots since they are economical, cost-effective, and most significantly, they encourage waste reduction. However, there is still a problem that must be solved regarding the production of high-quality C-Dots from biomass waste. Chemotherapy is currently recognized as the most successful way of cancer treatment, although it is known to induce severe side effects in patients due to its non-discriminatory harmful impact on both normal and tumor cells. The fundamental issue in cancer and other complicated disorders of chemotherapy is understanding drug distribution throughout organs and designing a site-specific drug delivery method that targets cancer cells. Therefore, it is of crucial importance to create advanced routes for the targeted and traceable administration of anti-cancer drugs. C-Dots can be produced using top-down or bottom-up approaches, with the latter method being more frequently employed for high-volume and low-cost syntheses. In this comprehensive review article, we mainly discuss the structure of CDs, classification of CDs, their properties, limitations, source of CDs, fabrication techniques, and characterization techniques. More significantly, we bring readers update on the most recent trends of CDs development in health care.

Sneha Desai K   Tarikere C.   and Taranath   

Nanotechnology is a rapidly growing field of medical research that may be used to a broad array of applications. Further, phytoconstituents are a promising possibility for the production of silver nanoparticles (AgNPs). AgNPs were biosynthesized using Haldina cordifolia bark extract and further characterization was done using UV-Vis Spectrophotometer, FTIR, XRD, DLS, Zeta potential and HR-TEM with SAED. The cytotoxic effect on lung cancer cell lines (A549) of AgNPs was studied by MTT assay and its antituberculosis activity was evaluated by MABA assay. The result showed that the AgNPs synthesized using bark extract of Haldina cordifolia have reported visible reddish-brown color and the absorption peak at 408nm (pH 10.5). FTIR confirmed the plant secondary metabolites that helped in green synthesis and capping of AgNPs. XRD revealed the crystalline nature of AgNPs. Zeta potential showed the stability at -42mV. HR-TEM and DLS images of AgNPs indicated the size ranged from 7 to 57nm. The dose response dependent anticancer activity was observed with IC50 value 17.64 µg/ml on A549 cell line which was more efficient than plant extract (IC50=79.92 µg/ml). On the other hand, AgNPs also showed promising antituberculosis activity with the MIC 0.4 µg/ml which was higher than the standard drugs used for comparison. We conclude that Haldina cordifolia is considered as an effective reducing and capping agent for green synthesis of AgNPs. Phytosynthesized AgNPs may subsequently be potential chemopreventive agent against the cancer treatment and as antituberculosis agent in future.

Manoj Singh   Vikas Kumar   Nisha Devi   Shivani Gupta   Mayank Raj   Sushil Kr Upadhyay   Vanita Thakur   Mukesh Yadav   and Nirmala Sehrawat   

Diabetes mellitus (DM) and its coupled comorbidities are a metabolic disorder that is highly prevalent and occurs in the body with high complexity of optimizing increase in glycaemic control because of decreased insulin activity or its low secretion. However, healthcare professionals have been going through the challenge of the mounting plethora of accessible healing options for minimizing hyperglycaemia. This has brought up a challenge responsible for creating difficulties in treating patients with therapeutic inertia. DM has basically been categorized into three sub-types, TYPE I DM, TYPE 2 DM and Gestational diabetes (GD). As TYPE I DM is usually treated through insulin replacement therapy, TYPE 2 DM is treated with various drugs. The highly effective drug therapy for TYPE 2 DM comprises many drugs such as Biguanides, Sulfonylureas, Thiazolidinedione, DDP-4, Alpha-glucosidase inhibitor, Combination therapy and GD treated with oral drugs. The combination therapy has been developed for those patients who cannot achieve routine therapeutic goals. In spite of the significant therapeutic profit, the conventional method has portrayed differential bioavailability and a short half-life period of the desired drug. The uses of such methods have greater side effects persisting with therapy ineffectiveness and patient non-compliance. Given the pathological complexity of the said DM, alternative approaches such as natural polyphenols and nanotechnology-based therapies are getting noticed, which certainly adds certain benefits for site-specific drug delivery with elevated bioavailability and reduced dosage regimen.

Snigdha Bhardwaj   and Sonam Bhatia   

Antimicrobial resistance has raised a serious concern due to the lack of therapeutics to control pathogenic infections. Pseudomonas aeruginosa is considered a multidrug-resistant pathogen and a leading cause of hospital-acquired infections. Anti-virulence approach mainly focuses on targeting bacterial virulence despite its growth and proves effective against such drug-resistant pathogens. In this study, we select a novel flavonoid compound, 7,8-dihydroxyflavone (DHF), which has been reported as a quorum sensing inhibitor (QSI) of P. aeruginosa, performed its in-silico studies to observe its binding affinity and potential interactions with the target protein (2UV0) and further developed it as a nano drug formulation (DHF-NF), and performed its in-vitro and in-vivo evaluation. The prepared DHF-NF was examined for its efficacy in the prevention of wound-associated surface infections of P. aeruginosa in rats. The DHF-NF was prepared by using homogenization and examined for several physical parameters. The prepared DHF-NF had a spherical shape and smooth topology. The microbiological assays demonstrated the inhibitory potential of DHF-NF in a dose-dependent manner. The histological analysis of Pseudomonas infected tissue of rat skin showed significant activity in animal group treated with DHF-NF as compared to control groups. The microbiological and in-vivo evaluation results revealed that the compound, DHF, showed strong inhibitory potential and suggest that the DHF-NF could be utilized as novel anti-QS and anti-biofilm therapeutics against Pseudomonal surface infections.

Gopinath Subramaniyan   Rajesh Pavan Ampapuram   Ramakrishnan Subburaya Rajendran   and Padamala Ramakrishna Reddy  

Background of the research and the purpose: Instead of using costly synthetic excipients or polymers, the authors were in search of an economical, easily available, and plant-based excipient for making microspheres. Plantago ovata seeds have already been proven to have anti-ulcer and gastro-protective activity. The same mucilage is used in this study as a polymer that can aid in floating the microspheres. In this study, mucilage from Plantago ovata seeds was added to sodium alginate and used with Metronidazole as a treatment to eradicate Helicobacter pylori. Methodology: Plantago ovata seed mucilage (POSM) and sodium alginate were used to make microspheres. To check the effects of independent variables (POSM and SA levels) on entrapment efficiency (EE) and floating time (FT) as responses, this paper used a central composite design with a design expert.11 software. The microspheres were investigated for Metronidazole (MNZ) content, size, yield, buoyancy, and release during congeniality studies. Results: As POSM content increased in the microspheres, MNZ entrapment increased, and the floating time (FT) was greater in microspheres with more POSM. MNZ release was slightly reduced in microspheres with higher levels of POSM. Conclusion: According to the investigation, MNZ can be retained in the stomach for extended periods of time in order to eradicate H. pylori, and the floating assets were enhanced by POSM.

M. Rajamiriyam   C. Anchana Devi   Farnaz Nabiya   and N. Pushpa   

Uterine leiomyomas are the most common benign gynaecological tumours that affect 50% - 60% of females belonging to reproductive age. The role of progesterone in the growth and development of leiomyomas is evident. Progesterone is regulated by progesterone receptors and it acts by activating PI3K/AKT pathway, by increasing proliferating cell nuclear antigen (PCNA) levels and Bcl-2 expression. Thus, modulating the receptor can help in the treatment of leiomyomas. The current study involves testing the efficiency of the various plant-based bioactive compounds to bind to the progesterone receptors, which may possess inhibitory or modulatory effects on or against progesterone receptors. These compounds can be further experimented with using other in vivo and in vitro methods to produce phytomedicine based on drugs for the treatment of uterine leiomyomas. This study is an in silico analysis performed using various bioinformatics databases and software. The receptor and ligand structures were retrieved from PDB and PubChem databases. Their pharmacokinetics and pharmacodynamics properties were analyzed using various databases. AutoDock4.2.6 was used for molecular docking, and the results were visualized using LigPlot+. Among 15 compounds selected, 8 compounds had higher binding energies than the control drug Ulipristal acetate i.e., -8.21Kcal/mol. Of which Ursolic acid, Vitamin-D2, and Betulinic acid had binding energies above -9.0 Kcal/mol. This concludes that these compounds can modulate the progesterone receptors, thus decreasing the proliferation and growth of uterine leiomyomas. Further studies can bring out the potential therapeutic effects of these bioactive compounds and they can act as a potential lead compound in the design of novel drug targets for the treatment of uterine leiomyoma.

Gamal A. Soliman   Mohammed A. Almutairi   Mohammad Ayman A. Salkini   Abubaker Hamad   and Maged S. Abdel-Kader   

Calligonum comosum Family Polygonaceae is a perennial shrub that grows in the desert areas in Saudi Arabia. The plant is extensively used for economic purposes and in Saudi traditional medicine. The plant is used for tanning hides and for wound. The current study aims to provide scientific evidence for the wound healing potential. The plant was extracted with methanol at room temperature and with water by decoction against two Gram-positive bacterial strains; Bacillus subtilis and Staphylococcus aureus, two Gram-negative bacterial strains, Escherichia coli and Klebsiella pneumonia, in addition to a pathogenic fungus Candida albicans. The methanol and water extract were formulated as creams and applied to evaluate the wound healing potential using rats as experimental animals. The methanol extract was more active in the antimicrobial testing and in accelerating the healing of wounds than the water extract. Wound healing potential was accessed via morphological parameters such as wound contraction, epithelization period and detailed as well as histopathological study of the healed skin. The wound was completely healed in the control group treated with Fucidin 2% cream after 18 days, while the methanol extract treated group reached 96.6% wound contraction in the same period. The water extract was much less active and in 18 gays resulted in only 73.2% wound contraction. Skin samples of methanol extract treated rats showed much improvement and almost normal appearance with normal content of collagen fibers, although slight weakness near the epidermis layer was observed. The obtained results strongly document the beneficial effects of C. comosum as wound healing activator and reveal the best method for the extraction of the plant.

T. Y. Pasha   C. Manojmouli   B. Ramesh   K. Naga Prashant   K. N. Purushotham   Noor Ul Eain   and M. Shankar   

Lung, prostate, and stomach cancer are the most prevalent cancers among males. Breast, colon, and cervical cancer are the most prevalent cancers among women. The literature also shows that patients suffering from cancer are increasing constantly, and hence the number of different chemotherapy treatments administered is increasing. The main objective of this review article is to summarize the effect of age on the half-life of some antineoplastic drugs belonging to the category of Topoisomerase inhibitors, alkylating agents, anthracyclines, purine analogs, antimetabolites, and N-nitrosoureas along with their pharmacokinetic properties. Literature indicates that highly bound antineoplastic drugs have higher differences in unbound drug concentrations among patients, and in some cases, the amount of concentration is not reflective of the unbound drug level and has an impact on pharmacokinetic parameters, including absorption, the volume of distribution, drug metabolism, and excretion. Protein binding affects the distribution and bioavailability of active drug substances.

Sowjanya Hatthi Belgal Mundarinti   and Hindustan Abdul Ahad   

Aim: The aim of the work was to explore the mucoadhesive properties of Mastic gum by involving it in mucoadhesive microspheres with Amoxicillin Trihydrate as a model drug. Using Carbopol-934P and varying amounts of Mastic gum. Methods: 9 interpretations of mucoadhesive microspheres were made by using Design expert software. A central composite design was applied to test the impact of independent variables (Carbopol-934P and mastic gum levels) on drug released at 10h and mucoadhesive strength as the response. Results: A congeniality and physical exam was conducted on the microspheres to see if Amoxicillin Trihydrate (ATH) was present, including its liberation. In formulations that contain lower levels of MG, mucoadhesion strength increased and drug released at the end of 10h was greater. Conclusion: Since MG acts as a release retardant, the amount of drug released is slightly reduced when higher levels are present in formulations. ATH gastro retention for eradicating with Mastic gum aided mucoadhesion (as this gum is proven H. pylori activity) is capable of completely capturing the gastrointestinal tract and effectively delivering the medication to the stomach.

Kenechukwu Obikeze   Garth Gainsford   Maajidah Kamaar   Rhulani Mbewe   Michaela Palmer   and Nazeerah Wilsnach   

Cathepsin cysteine proteases such as cathepsin S are responsible for the unfavorable and irreversible dysregulation of extracellular matrix (ECM) proteolysis found in cardiomyopathy, heart valve diseases and atherosclerosis. Cathepsin S plays a central role in ECM remodeling, which has been implicated in the development and progression of cardiovascular diseases. The current study aimed to evaluate the aqueous and ethanol extracts of the berries of Crataegus monogyna and the leaves of Centella asiatica for inhibition of cathepsin S activity using an in vitro fluorescent assay. Dried and ground berries of Crataegus monogyna and the dried and ground leaves of Centella asiatica were used to prepare the aqueous and organic extracts. A fluorometric enzyme assay was used to evaluate the inhibition of cathepsin S by the plant extracts. The aqueous extracts of Crataegus monogyna and Centella asiatica produced a maximum enzyme inhibition of 6% and 9.6% respectively, at a maximum of 200 ÎĽg/ml. The organic extract of Centella asiatica produced a maximum inhibition of 14%, occurring with the 100 ÎĽg/ml concentration. The ethanol extract of Crataegus monogyna produced a concentration-dependent inhibition of cathepsin S enzyme activity for all concentrations, with a maximum inhibition of 71.7% obtained with the highest concentration of 200 ÎĽg/ml. This demonstrates that the organic extract of Crataegus monogyna plays a crucial role in the inhibition of cathepsin S in vitro and could serve as a viable source for the isolation of cathepsin S inhibitors.

Ganesh Sampat   Shailendra S. Suryawanshi   Mahesh S. Palled   Archana S. Patil   Pukar Khanal   and Abhijeet S. Salokhe   

The current drug research techniques, combinatorial synthesis and high throughput screening, help in obtaining and pre-evaluating thousands of compounds in a short duration of time. Among the selected compounds, the best hit molecule becomes the lead, and the drug likeness property helps to optimize the selection. Lipinski's Rule of five is the most widely used filter in pre-evaluation of compounds, according to Lipinski's Rule of five the molecule with poor oral absorption and low permeation has the molecular weight >500, ClogP >5, hydrogen bond acceptor more than 10 and hydrogen bond donor more than 5. To evaluate the Rule of Five, the top selling drugs of 2018-19 were selected. Among the selected 56 drugs, 12 drugs (tenofovir disoproxil, sofosbuvir and ledipasvir, sofosbuvir/velpatasvir, trastuzumab, glecaprevir, pegtilgrastion, Lumacaftor/ ivacaftor, fluticasone propionate and salmetarol, elbasvir, darunavir ethanolate, Linagliptin, metformin, fluticasone furoate and vilanterol) did not fulfill the rule. The rule is very useful in selecting the better compound in chemolibraries, but should be used carefully and with certain criterion due to possible exclusion of promising compounds.

Kannan O. Ahmed   Imad Taj Eldin   Mirghani Yousif   Ahmed A. Albarraq   Bashir A. Yousef   Nasrein Ahmed   and Anas Babiker   

Clinical pharmacists are in a suitable position to improve medications adherence for chronic diseases, including heart failure (HF). This study aimed to identify if the structured educational intervention by the clinical pharmacist can improve adherence to HF medications in a specialized HF clinic. Methods: A quasi-interventional study was implemented in an outpatient HF clinic for six months at Ahmed Gasim Cardiac Surgery and Renal Transplantation Center, Khartoum, Sudan. Adherence was assessed by using Morisky-4 Medication Adherence Scale (MMAS-4). Clinical pharmacist intervention using verbal and written materials composed of different aspects to promote medications adherence for HF were performed during the study period. Results: Among 110 patients, 97.3% were non-adherent to HF medications at baseline, with the exception of receiving education about HF; all sociodemographic and clinical characteristics of patients were not associated with the non-adherence status. Significant improvement in medication adherence was reported after clinical pharmacist intervention by different views of MMAS-4. There was a reduction in the total mean MMAS-4 score (2.64 ± 1.1 vs. 0.67 ± 0.9, P=0.001), and a significant increase in the percentage of patients having high adherence (2.7% vs. 56.4%, P=0.001) before and after clinical pharmacist intervention. By contrast, the proportion of patients with medium and low adherence was significantly reduced after intervention (42.7% vs. 37.3%, P=0.001) and (54.5% vs. 6.4%, P=0.001), respectively. Conclusion: Non-adherence was highly prevalent among Sudanese patients with HF; the clinical pharmacist led-educational intervention can improve medication adherence for HF medications.

Mohammad Y. Abajy   Ream Nayal   Mahassen Alqubaji   and Yara Abdrabbo   

Cyclophosphamide is a very important chemotherapy drug for patients with cancers and autoimmune diseases, but unfortunately it is a mutagenic and cytotoxic agent. In this research, the effectiveness of black cumin (Nigella sattiva) seeds hydroethanolic extract in reducing cyclophosphamide-induced genotoxicity was studied after determining the safety of this extract. The acute and subacute toxicity of the extract was evaluated at a dose of 1500mg/kg/day in albino rats. The extract did not lead to any deaths or behavioral pattern changes in rats, in addition, the biochemical analysis and the results of the relative organ weights showed the absence of any toxicity for the extract. The anti-mutagenic ability of the extract was evaluated using in vivo chromosomal aberration test and in vitro comet assay. Results showed that oral administration of the extract to rats before treatment with cyclophosphamide caused a significant decrease in chromosomal aberrations. In comet assay, the extract showed also signi�cant reduction in cyclophosphamide-induced DNA migration. It could be concluded that black cumin seeds extract had a protective effect against Cyclophosphamide - induced genotoxicity and may be considered as an anti-mutagenic agent after conducting more studies.

Haranath Chinthaginjala   Hindustan Abdul Ahad   and Bhupalam Pradeepkumar   

In the present study, the main objective was to develop and evaluate a novel floating mucoadhesive drug delivery system for famotidine. In order to deliver drugs in accordance with circadian behavior, continuous drug delivery systems were developed. It represents that these systems will deliver the drug when the patient's condition is at most risk. The combination of floating behaviour with the formulation improves the gastric dosage residence. The method adopted for the preparation of tablets was press coating technology. Here it has two layers: a core layer and a coat layer. The core layer consists of active ingredients, and the coat possesses gas-generating agents and polymers like HPMC, Carbopol, and Pectin. The formulations were characterised for weight variation, friability, hardness, disintegration of core tablets, in vitro drug release studies and Ex vivo mucoadhesive studies. All the formulations manifested better results in terms of floating lag time, floating time of more than 8 hours and good adhesion property. The formulation F6 manifested drug release of 99.42% at the end of 7 hours. It was concluded that the formulation F6 is the best formulation which accomplishes the anticipated release with specific lag time and has the ability for off release followed by burst release which can effectively suppress nocturnal histamine level and hence suppress high nocturnal acid release.

Sowjanya Hatthi Belgal Mundarinti   and Hindustan Abdul Ahad   

Aim: Searching for a new polymer that can be used in pharmaceutical formulation is a laborious and cost oriented practice. To resolve this, researchers are in search of a cost-effective and reliable excipient. Synthetic polymers are costly, whereas natural ones are abundant and economical. In the same way, discovering a new drug is a horrendous process with time, cost, and approval. The study's goal is to investigate Mastic gum's mucoadhesive properties by incorporating it into mucoadhesive microspheres with Amoxicillin trihydrate as a model drug. Methods: Nine interpretations of mucoadhesive microspheres were made with carbomer 934P and varying proportions of mastic gum (MG). A central composite design with design expert software is used to check the impact of independent variables (mastic gum and carbomer 934 P levels) on entrapment efficacy and mucoadhesion time as the responses. As part of congeniality studies, the microspheres were examined for amoxicillin trihydrate (ATH) content and liberation. Results: Good quality microspheres were formed that showed suitability with the excipients and possessed appreciable outcomes for the tests conducted. The study expressed the equation for ATH entrapment as +82.70+0.1333A+6.40B+0.0500AB+ 0.0000A₂-2.80B₂ and the mucoadhesion time as +13.10+0.2500A+1.42B-0.0500AB+0.1500A₂+0.1500B₂. These equations indicate the impact of independent variables on the response studies. These equations discovered that ATH entrapment increased with an increase in MG levels in the formulations and that the mucoadhesion time was greater in formulations with higher MG levels. In formulations containing higher levels of MG, the drug release is slightly reduced. Conclusion: The study summarized that amoxicillin trihydrate is capable of good stomach-specific drug delivery by carbomer 934P and enhanced by mastic gum when prepared as mucoadhesive microspheres that are cost-effective, operational, and stable. This approach also resolves the gastric retention of ATH to eradicate H. pylori and the mastic gum has proved an anti-ulcer possession.

Lalitha Vivekanandan   G. S. Sri Bharathi   Jagadeeswaran Murugesan   Kiruthiga Natarajan   and Sivakumar Thangavel   

Background: Alzheimer's disease (AD) is a common nerve problem that leads to memory loss, particularly in the elderly. A shortage of acetylcholine in the brain, as well as oxidative stress, induces Alzheimer's disease. Currently, limited drugs are available to treat Alzheimer's disease because continuous use of these medications causes several side effects. Hence, we need high efficacious drugs to treat Alzheimer's disease with fewer side effects. Sapindus emarginatus Vahl or soap nut is a member of the Sapindaceae family. It's been used traditionally as an antiepileptic, antipruritic, antifertility, antiemetic, and anti-inflammatory agent. It is cheap, widely available, and reported to counteract chronic diseases linked to oxidative stress, such as ulcers and dyslipidemia. Objective: The purpose of this study was to determine the anti-Alzheimer and antioxidant properties of ethanolic seed extract of Sapindus emarginatus (ESSE) against scopolamine-induced amnesia. Methods: The total flavonoid level of the ESSE was estimated by a UV-visible spectrophotometer. The scopolamine (1 mg/kg/PO) was administered as a single intraperitoneal injection on the seventh day for induction of dementia in mice. The ESSE (250 and 500 mg/kg/PO) and donepezil (2.5 mg/kg/PO) was administered orally for 7 days. The neurobehavioral tests such as an elevated plus maze, radial arm maze, and Y-maze tests were undertaken for estimation of behavioral trials. The brain homogenate was used for the estimation of acetylcholine, acetylcholinesterase, and oxidative cell injury markers such as MDA, LH, SOD, CAT, and GSH. Results: The total flavonoid content of the extract was 0.47 mg of QE/g. Scopolamine degraded memory, as well as caused alterations in acetylcholine, acetylcholinesterase, and elevated oxidative stress in the brain. Pretreatment with ESSE reduced scopolamine-induced behavioral, neurochemical, and oxidative stress markers. Conclusion: The ESSE has an anti-amnesic impact, making it an attractive option for targeting multiple events as a possible technique to slow cognitive impairment.

Utkarsh Kaushik   and S. C. Joshi   

Background and Objective: Nanotechnology has spread its roots and branches covering every field. Fascinating physcio-chemical properties and functional applications have made zinc oxide nanoparticles (ZnO NPs) one of the most multifaceted materials. Zinc oxide nanoparticles synthesis using concoction of plant is safer and nature cordial due to its non-toxic and clean compared to its chemical counterpart. Present quest involves zinc oxide nanoparticles production by chemical and biological methods (Citrus sinensis peel extract). Materials and Methods: Synthesized zinc oxide nanoparticles were characterized using ultraviolet-visible UV-Visible spectroscopy, Fourier transform infra-red (FTIR) spectroscopy, and scanning electron microscopy (SEM). Synthesized zinc oxide nanoparticles at concentration (0.1g, 0.25g and 0.5g/10ml) were compared against microbial strains Staphylococcus epidermidis and Aspergillus flavus. Results: Synthesized ZnO NP's shows absorption peak at 356 nm in case of biological synthesis and 386 nm in case of chemical synthesized. FTIR proves the presence of alcohol, phenol, nitro compound; alkyne in case of biologically synthesized ZnO NPs and alkene, alkane, alkyl halides in case of chemically synthesized ZnO NPs. SEM confirmed the average size of 25-40 nm. Further, promising results were obtained at 0.5g/10ml of biologically synthesized ZnO NP's in case of Aspergillus flavus and Staphylococcus epidermidis. Conclusion: the biomimetic synthesis of ZnO nanoparticles could be an alternative to chemical synthesis and commercially available drugs.

Vijaya Vichare   Vishnu Choudhari   Vrushali Tambe   and Shashikant Dhole   

Prior knowledge of chemical stability of drugs directs path for right selection of dosage form, excipients, storage conditions and packaging material. Literature survey revealed that, there are analytical methods reported for quantification and stability indication of Canagliflozin in bulk and formulation. But there is not much information available about the degradation products generated under different stability conditions. With this background, characterization of oxidative degradation product of Canagliflozin was successfully carried out by Liquid Chromatography-Mass Spectrometry (LC-MS/MS) studies. Degradation product was generated by forced degradation, according to International Conference on Harmonization (ICH) guidelines. Degradation product was separated from Canagliflozin by validated reverse phase (RP)-HPLC method using C18 column and Acetonitrile: Water pH 3.0 adjusted with 0.1% formic acid (70: 30, v/v) as mobile phase at a flow rate of 1mL/min. The developed RP-HPLC method was validated for different parameters as per ICH guidelines. The method was found to be linear in a range of 25-225 μg/mL. The developed method was found to be specific, accurate, precise, sensitive and robust. The marketed tablet formulation was analyzed by the developed method and the percent drug content was found to be 100.09 ± 1.96 % w/w. Separated degradation product was characterized by LC-MS/MS studies. From LC-MS/MS data probable structure of the degradation product was interpreted and the mechanism of degradation was proposed. The probable structure of degradation product was proposed as2-(4-Fluorophenyl)-5-({2-methyl-5-[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]phenyl}methyl) thiophene-1-one. The mechanism of degradation was proposed by S-oxidation of thiophene ring to form thiophene oxide. This information will help synthetic chemists to design a synthesis scheme for the oxidative degradation product, which can be used as a reference standard for impurity profiling. It is also suggested to protect CN from oxidative conditions for improved stability.

Seema S Rathore   Navyashree G A   Komala M   Chinju Susan Chacko   and Shravya Lakshmi S   

Diet and lifestyle of an individual play a major role in maintaining the health of an individual, and any variation associated with these two factors would lead to serious consequences. Polycystic ovarian syndrome is one such condition which is an endocrine disorder observed in teen aged and premenopausal women in modern world, where there is formation of cysts on the ovary/ ovaries. It may be due to increased secretion of androgen, imbalance in doshas (vata, pitta and kapha), improper diet and lifestyle. There are various medicated and non-medicated therapies available for reducing the symptoms and conditions associated with poly cystic ovarian syndrome. Medicated treatment involves maintenance of hormonal balance, Type II diabetes mellitus, infertility, synchronisation of the vata, pitta and kapha, insulin resistance, regularization of menstrual cycle, reduction of acne and hirsutism and these are done by administration of allopathic and herbal formulations. Non-medicated treatment includes surgery by which cysts are removed and also by acceptance of healthy lifestyle. This review centres on providing information regarding the medicated and non-medicated treatment available for treating the type of conditions and symptoms consorted with poly cystic ovarian syndrome along with their pros and cons.

Swetha Jose   Anitta Merlin Augustine   Anvy Thankachan   Meby Susan Mathew   and Bazil Alias   

Context: Ever since the introduction of apremilast in the Indian market in 2017, it was used in psoriatic arthritis with little information on the benefits of apremilast in this population, especially regarding the tolerability of the patients to tapered doses of apremilast. Aims: This study evaluates the efficacy, safety, and tolerability of apremilast in psoriatic arthritis. Settings and Design: A retrospective study was conducted on 120 patients aged ≥18 years who regularly visited one of the largest standalone rheumatology clinics between November 2018 and September 2019. Methods and Material: The proportion of patients who improved by 50% in their psoriasis area and severity index (PASI-50) score, as well as the reduction in tender joint count, swollen joint count, patient global health evaluation, and erythrocyte sedimentation rate, were all evaluated as effectiveness objectives. Statistical Analysis Used: The non-parametric test, Wilcoxon signed-rank test was used to compare between the baseline and follow-up measurements. Results: From a total of 120 patients, ninety-five patients showed a 65.09% reduction in the PASI score in the 16th week. A mean value for bath ankylosing spondylitis (BASDAI) of 4.36 at baseline was significantly reduced to 1.73 by the 16th week. Common adverse effects reported were gastritis (38.2%), diarrhea (32.4%), and fatigue (26.5%). Conclusions: Because of its tolerance and safety profile, apremilast may be regarded as a helpful medicine for the treatment of psoriatic arthritis, either alone or in combination with other medications, according to the findings of the study.

Sabari Anandh J V   Manimekalai K   Rajendra Kumar A   and Bragadeeswaran S   

Background: Algae are an excellent wellspring of biologically active secondary metabolites and have been shown to exhibit a wide range of therapeutic properties. Several Asian cultures have a strong tradition of utilizing various seaweeds extensively in cooking as well as in herbal medicines preparations. Their use in traditional medicine has been reported since time immemorial. Aims and Objectives: To evaluate the analytical specification, proximate analysis, and trace elemental analysis of Kadarpassi Chooranam. Methods: Halimeda gracilis (green alga) was collected from the Mandapam region and identified by a marine biologist. Halimeda gracilis was made into chooranam, and it was purified by using the 'Avi Enthiram' method and analytical specification, Proximate analysis, and trace elemental analysis were performed. Results: Kadarpassi Chooranam was standardized as per PLIM guidelines testing protocol, the Heavy metals were found within the normal range, Aflatoxin, Pesticide residues, Organochlorine, Organophosphorus, and Synthetic pyrethroids were found to be below the limit of quantitation (BLQ) and the microbiological test showed free of harmful pathogen. Trace elemental analysis and proximate analysis of Kadarpassi Chooranam showed significant presence, which can be used as health supplements. Conclusion: Kadarpassi Chooranam contains the permissible level of heavy metals, toxins and is free of harmful pathogens. The chemical constituents of the chooranam were characteristically studied, which showed that they contain organic compounds, which may have various pharmacological activities. So, Kadarpassi Chooranam is the first of its kind in the medicinal field. Future studies (in vitro and in vivo) will explore the potential medicinal properties.

Mohamed Abdellatif   

Venous thromboembolism (VTE) is reportedly the second common cause of death among cancer patients. Management of VTE with low molecular weight heparins (LMWH) and Vitamin K antagonists (VKA) is associated with significant clinical challenges that led to the emergence of direct oral anticoagulants (DOAC) as an alternative for the management of cancer-associated thrombosis (CAT). The objective of this review is to provide an updated review of the completed and upcoming randomized controlled clinical trials (RCT) comparing the safety and efficacy of DOAC versus LMWH in the management of CAT in adults. A comprehensive literature survey was conducted till 7th January 2021 to review the completed randomized controlled clinical trials (RCT) comparing the safety and efficacy of DOAC versus LMWH in the management of CAT in adults. In order to search for upcoming trials, the Cochrane library and clinicaltrials.org databases were surveyed until the same period. The author found four completed RCT of DOAC in the management of CAT. Apart from these, there were another four RCT that are either ongoing or are yet to publish data. DOAC were reported to be noninferior to LMWH in the treatment of cancer-associated thrombosis in cancer patients with low bleeding risk and without gastrointestinal or gastrourinary cancers. Among patients with gastrointestinal or gastrourinary cancers and VTE, LMWH are preferred.

J. Josephine Leno Jenita   Jahnavi Kulkarni   Agasa Ramu Mahesh   Shanaz Banu   Seema S. Rathore   and Manjula D   

Protein kinases play a prominent role in transferring a phosphate group from ATP (adenosine triphosphate) to serine, tyrosine, or threonine residues. Mutation and dysregulation in their activity lead to an imbalance in the health causing diseases like cancer. Protein kinase inhibitors have proved to be more effective in addressing such impairment caused by the dysregulation of protein kinases. Several protein kinase inhibitors like antibodies and small molecules have been approved by the regulatory bodies like US FDA, and many of them are being developed and expected to enter the clinical trials and subsequently to the market in the near future. However, targeting such kinase inhibitors to the desired site of action remains a challenging process. The current review focuses on the applicability of Nano platforms for targeting protein kinase inhibitors to the desired site of action and thus enhancing the therapeutic efficacy of the drug molecules against cancer. Besides, it also gives a brief idea to the readers about the imaging nanoplatforms investigated for the detection of protein kinase inhibitor activity along with the list of ongoing clinical trials pertaining to protein kinase inhibitors.

Anbuchellvam   and Jayalakshmi G   

Inflammation is an important part of the body's defense system, since it helps to remove and repair damaged tissue as well as neutralize poisonous compounds. The cascade includes increased permeability in microvessels, the attachment of circulating cells to vessels near the damage site, migration of various cell types, and the formation of new tissue and blood vessels. The analgesic and anti-inflammatory effects of rosuvastatin and telmisartan were examined in albino rats and Swiss mice. The hot plate approach regarded licking and leaping as response points. The combo group and rosuvastatin had similar analgesic efficacy. Its analgesic efficacy was significantly lower than that of a normal analgesic aspirin. Telmisartan, too, showed no analgesic effect. In this experiment, the percentage of inhibition at 120 minutes revealed that rosuvastatin and telmisartan given alone had a favourable impact on acute inflammation. Furthermore, the decrease of acute inflammation in the combination group was equivalent to that of aspirin. The data demonstrated that the capacity of the combination group to reduce chronic inflammation is equivalent to that of aspirin as an anti-inflammatory drug.

Nisha Khatik   

A nanoparticle (NP) is a microscopic particle with a length of two or three dimensions greater than 0.001 micrometer (1 nanometer =10^�9 metre). NPs may be classified into different classes based on their specific properties, shapes or sizes, and high surface area-to-volume ratio. Nanoparticles have a remarkable capacity as 'magic bullets' stacked with herbicides, fungicides, supplements, fertilizers or nucleic acids, specializing in expressing plant tissues to deliver their charge to the appropriate piece of the plant to perform desired outcomes. The smart design and synthesis of a library of nanomaterials, exact control over their physicochemical properties and simplicity of their surface functionalization to assemble explicitness is to be certain fundamental for the achievement of disease treatment and harmfulness in the biological systems. Green techniques for nanomaterial synthesis observe natural organic systems to nanomaterial production. Green synthesized nanomaterials are at present powerful and significant tools for protecting the drug from the dangerous surroundings in addition to overcoming the organic obstacles to access of the drug in targeted tissues and dealing with drug resistance. NPs were extensively utilized in numerous biomedical applications, site-specific drug delivery systems and cellular uptake because of their inert nature, stability, high dispersity, non-cytotoxicity, and biocompatibility. Nanoparticles may be programmed for recognizing the cancerous cells and giving selective and correct drug delivery avoiding interaction with the healthy cells. However, usage of those NPs is restrained through factors like lack of stability in adversarial environment, concerns regarding bioaccumulation and toxicity, need of relatively trained employees for device assembly and operation, and problems with reproducibility and affordability.

Hemanth Annepogu   and Hindustan Abdul Ahad   

Aim: The primary objective of the study is to evaluate solid dispersion (SDs) made into tablets containing Etoricoxib (ECB) and Thiocolchicoside (TCS) for different in vivo parameters and in vitro drug release as an extension of the work described by Annepogu et al., in 2018. Methods: The in vitro study was constructed on various evaluation parameters of SDs of ECB and TCS. From earlier study results, we have selected formula-5 SDs of ECB and TCS for in-vivo study and comparison with marketed ones. Results: Plasma drug availability was performed on 6 healthy rabbits of both sexes (weighing 2.0-2.5 kg). They were aimlessly alienated into 2 groups of alike size by parallel design. Later, the study was HPLC analysis of the drug in the plasma, which involved preparation of the spiked plasma sample, and an analytical technique was established (simple and cost-effective method for ECB and TCS simultaneous estimation). The plasma samples were assessed for pharmacokinetic parameters. Finally, the F-5 formulation was assessed for in vitro drug release by comparison with the marketed preparation (Recox tablets-Hochest Biotech India). Conclusion: The study summarizes that TCS and ECB reached systemic circulation better than the pure drugs, and the kinetic values were appreciable. The drug discharge from the SDs was identical to the marketed one.

Sivananthan Manoharan   Adawiyah Suriza Shuib   Noorlidah Abdullah   Nor Farrah Wahidah Ridzwan   and Saharuddin Bin Mohamad   

Hypertension is one of the most common chronic diseases affecting millions of people worldwide. The structure-based drug design targeting domains of the ACE is important in the treatment of hypertension. The domain specificity inhibition of somatic ACE and testicular ACE by tripeptide GVR by binding to the specified active site of ACE has not been previously described. From this study, it was shown that tripeptide GVR was significantly bound to the active site of the C-domain of somatic ACE as compared to the N-domain. Although tripeptide GVR was mimicking captopril, a strong inhibition of the C-domain's active site and a weak inhibition of the N-domain by GVR probably led to less significant side effects to the patients as compared to the strong non-domain specific inhibitor, captopril. Besides, the ability of tripeptide GVR to strongly inhibit testicular ACE was also shown. From this study, it has been shown that tripeptide GVR was able to bind on both somatic ACE and testicular ACE. It was also shown that the existence of arginine amino acid at the C-terminal of a peptide sequence was essential to inhibit ACE significantly.

Shadab Ali   Amar Singh Kashyap   and Anuradha Singh   

The drug plants are inevitably consistent in view of other compositions and the standardization. They are influenced by many factors, such as surrounding environment, harvesting, storage and processing. The packaging also plays an important role in maintaining the quality and efficacy of the herbal drugs. The proper packaging and storage maintain the quality of herbal crude drugs. The storage specificity was studied on Boerhavia diffusa Linn. And the effect of fungal infection on stored plant material in different packaging was found. In the study, four different types of packaging were taken to observe the quality and efficacy i.e., polythene, cloths, paper and gunny bag. One unpacked sample was used as a control set. It was a two-year study observed from December 2018 to December 2020. The total number of mycoflora was found on Boerhavia diffusa Linn material in variable number in different seasons. In 2019, there were 15 species in April, 24 species in August and 4 species in December. In 2020, there were 3 species in April, 7 species in August and 0 in December. The total number of 33 different fungal species belonging to 15 genera was recorded on all packaging. 12 species belong to Aspergillus, 01 Alternaria, 01 Botrytis, 01 Botryodiplodia, 01 to Curvularia, 01 to Colletotrichum, 03 to Fusarium, 02 to Gilmaniella, 01 to Moniliella, 01 to Mucor, 03 to Penicillium, 01 to Paecilomyces, 03 Rhizopus, 01 to Thelavia and 01 to Zygosporium species. The polythene packaging and cold winter climate were the best for the least microbial attack and minimizing the loss of quality of studied crude drugs.

Uma Sankar Gorla   GSN Koteswara Rao   Rajasekhar Reddy Alavala   Ravi Manne   and Kadiyala Harshitha   

In the current investigation, the selected phytocompounds of Cocculus hirsutus were screened for potent tau aggregation inhibitors for Alzheimer's disease through in silico molecular docking. Approximately 19 phytocompounds from Cocculus hirsutus were selected and assessed for their drug likeness based on rule-of-five using Swiss ADME. The phytocompounds that passed rule-of-five were subjected to in silico analysis through molecular docking on Cyclin-dependent kinase 5 (CDK5) and Glycogen synthase kinase 3 beta (GSK3B) using Molegro Virtual Docker v6.0. Molecular docking studies. The molecular interaction on CDK5 and GSK3B enzymes indicate their role in the tau protein aggregation inhibitory activity of the phytocompounds. In silico analysis showed that hirsutine and cohirsinine bind effectively at the active site of target proteins with a MolDock score of -115.08 and -107.29 respectively. The MolDock scores, ReRank scores and interaction poses of the phytocompounds were compared with the known inhibitors of CDK5 and GSK3B enzymes. The present research created a new perspective in understanding hirsutine and cohirsinine phytocompounds as effective inhibitors of tau aggregation and further research in vitro and in vivo may confirm their therapeutic potential in Alzheimer's.

Jincy Thomas   A. Srinivas   and Folitartha Roy   

The current research has been performed to substantiate the traditional claim of the anti-diabetic activity of seeds of Datura Innoxia Mill. in rats. This plant contains scopolamine alkaloid, which has been reported to be used in operations as pre-anaesthesia, used in delivery, as well as in ocular surgeries and for travel sickness prophylaxis. Datura is a medicinal and hallucinogenic plant that is used everywhere in the globe. Datura is revered in Ayurveda because all parts of the plant have medicinal properties, including the roots, leaves, seeds, and flowers, and have been employed to treat a variety of ailments, including leprosy, rabies, and insanity. Withanolide has recently been found to have potent anti-tumor, anti-inflammatory, anti-bacterial, hepatoprotective, soporfic, cytotoxic, and immune suppressant properties. An alloxan-induced diabetes model in rats was used to test the anti-diabetic activity of an ethanolic extract of the seeds of Datura Innoxia Mill. (Family-Solanaceae). A comparison was made between both the animals treated with extract from seeds and animals treated with known drug for diabetes i.e.., glibenclamide. The extract dose was chosen based on acute oral toxicity tests conducted in accordance with OECD norms. The outcomes revealed the fact that ethanolic extract significantly reduced the glucose levels in blood. The findings supported the use of seeds extract in the treatment of diabetes.

Naveen Kumar Kudure Jayanna   Venkatesh   Pradeepa Krishnappa   and Santosh Kumar Shimoga Rajanna   

Lantana camara is considered as a notorious weed and a popular ornamental plant. It has been observed since ancient times because the plants are an excellent source of medicine. Lantana camara has long been considered one of the most important medicinal plants in the world. Lantana camara is used in traditional medicine to treat cuts, swelling, ulcers, cataracts, biliary fever, itching, eczema and rheumatism. Different parts of the Lantana camara plant are used to treat colds, headaches, whooping cough, asthma, chicken pox, bronchitis, eye lesions, and high blood pressure. Lantana camara has been scientifically studied for various therapeutic activities like antibacterial, antioxidant, antipyretic, insecticidal, antimicrobial, wound healing etc. Various literatures have reported the phytoconstituents present in all parts of Lantana camara. In the current study, phytochemical analysis and antimicrobial activity of leaves and stem of Lantana camara were studied. The phytochemical analysis using chloroform and ethanol extracts for phenolic acids (Gallic acid) and flavonoids (Quercetin, Myricetin) by HPLC method in stem and leaves of Lantana camara. The present study evaluated the antimicrobial activity of ethanol and chloroform leaves extract against some pathogenic bacteria and fungi by using agar well diffusion method. This study can be concluded that Lantana camara of steam and leaves are comprised of bioactive compounds which possess antimicrobial activity against pathogenic bacteria and fungi.

Abhishek Kumar Pandey   

Since the beginning of humankind, people are using numerous plants to cure diseases and abnormalities. Bacopa monnieri has been used by people for a long time. This plant has several medicinal and biochemical properties which would be beneficial to treat diseases. The current review article summarizes the medicinal, presence of the bioactive compound, mechanism of action, therapeutic importance, clinical trials, ethnobotanical usage, and distribution of the plant with respect to India and worldwide. Relevant information and literature on Bacopa monnieri were extracted from different sources and their finding were discussed in the manuscript. The number of therapeutic properties of the plant has been seen in the animal model experiment including anti-diarrheal, antioxidant, anti-inflammatory, anti-cancer, anti-fungal, anti-bacterial, anti-convulsant, hepatoprotective, antiulcer, anti-depressant, anti-hyperglycemic and anti-nociceptive activity, immunostimulatory activity, and wound healing activity. This article recapitulates ethnopharmacological uses of Bacopa monnieri to explore its therapeutic potentials thereby providing a basis for future research. Bacopa monnieri exhibits a comprehensive of pharmacological activities that could be observed by the presence of a vast range of chemical constituents. Manuscript also comprises tissue culture techniques and propagation of Bacopa monnieri. The study also provides a descriptive outlook on the uses of Bacopa monnieri in wastewater treatment. This review article highlights the endless possibilities present in the plant and also sheds light on research that has not yet been done on this plant and may prove useful if done in the future.

Chandra Shekar Singh   and Papiya Bigoniya   

Aims: Cichorium intybus L. is traditionally used for the management of the various liver disorders and also widely scientifically reported for hepatoprotection. The present study aims at investigating cichotyboside, bioactive sesquiterpene glycoside, from seeds for hepatoprotective effect against carbon tetrachloride (CCl₄) following isolation and characterization. Methods: Cichotyboside was isolated from C. intybus seeds and characterized by infrared spectroscopy (IR), liquid chromatography-mass spectrometry (LC/MS), and carbon 13 nuclear magnetic resonance (¹³C NMR). High-performance liquid chromatography (HPLC) and high-performance thin-layer chromatography (HPTLC) have been developed for the standardization of Cichotyboside. In this study, biochemical assays, liver functional capacity restoration regarding drug metabolism, antioxidant potential, and histological staining were applied to evaluate the anti-hepatotoxic efficacy of cichotyboside on a carbon tetrachloride induced liver injury in rats. Results: The results showed that cichotyboside could significantly attenuate the pathological changes, increase the levels of hepatocyte repair, and regulate oxidative damage. Hepatoprotective activity of cichotyboside is indicated by its ability to decrease thiopental induced sleeping time, increased BSP clearance, reverse effect of CCl₄ on the body weight, relative liver weight, serum liver function parameters, histopathology and activity of liver antioxidant enzymes. Conclusion: Cichotyboside exerts hepatoprotective activity against the CCl₄ induced toxicity, possibly by its remarkable antioxidant potential, reversing the impaired metabolisms and repairing the fatty changes in hepatocytes.

Jesanto Mathew   Chakrakodi Shashidhara Shastry   and Sharad Chand   

Introduction: Leucaena leucocephala is a commonly used plant in the Ayurveda system of medicine to alleviate several ailments. Different parts of Leucaena leucocephala are used for the treatment of ailments such as diabetes, ascariasis, intestinal parasitism and trichinosis. It is also used as an emmenagogue, emollient and as nutritious forage for cattle. Objective: This study was conducted to evaluate the plant extract's effect on memory and learning using in-vivo models and ex-vivo models. Methods: The plant extract was prepared by using the Soxhlet extraction procedure. The effect of the extract on nootropic activity was assessed against scopolamine-induced amnesia using different exteroceptive models such as Elevated plus maze, Y maze and Hebb William's maze. Acetylcholinesterase activity of the rat brain homogenate was estimated using Ellman's method. The activity of the extract was compared with the standard drug piracetam. Results: On pre-treatment with ethanolic extract of L. leucocephala, in-vivo studies showed significantly improved spatial learning and memory against scopolamine-induced amnesia in Wistar rat models in a dose-dependent manner. Ex-vivo studies of rat whole brain homogenate showed a significant decrease in acetylcholinesterase activity in extract-treated animals. Conclusion: The ethanolic extract of the leaves of L. leucocephala showed significant nootropic potential against animals induced by amnesia using scopolamine.

Ashwini Gawade   Sanjay Boldhane   Anil Pawar   Rohini Pujari   and Ashwin Kuchekar   

Dabigatran Etexilate Mesylate (DEM), a salt of prodrug dabigatran etexilate, is a potent, oral, reversible and direct thrombin inhibitor with low oral bioavailability. The present research investigation focused on the formulation of immediate release (IR) tablets of DEM cocrystals and evaluation of In vivo anticoagulant activity. The results of the study showed that the formulated IR tablets of DEM showed improved efficacy in comparison with the plain drug by enhancing the pre-compression parameters such as bulk density, tap density, Carr's index, angle of repose and Hausner's ratio and post-compression parameters like thickness and weight variation, hardness and friability, In vitro dissolution parameters. The improved efficacy was confirmed by improvement in the pharmacodynamic parameters such as cutaneous bleeding time and clotting time indicative of enhanced bioavailability of dabigatran. Thus, it can be concluded that the IR tablets of dabigatran cocrystals can be proven to be more effective in producing the anticoagulant effect in clinical practice as compared to the plain drug resulting in more patient compliance.

Sonam Bhutia   Bibhuti Bhusan Kakoti   and Prosanta Pal   

The novel coronavirus disease is a rapidly spreading infection caused by recently discovered different variants of SARS CoV-2 viruses, causing mild to severe respiratory symptoms in the majority of people. The Coronavirus disease 2019 pandemic has spread almost all the nooks and corners of the world. There are significant possible approaches pharmaceutically to fight against COVID-19. Original full-text research articles were searched online in PubMed, ScienceDirect, ResearchGate, Google Scholar, Core and Wiley Online Library. Scientists throughout the world are working on different platforms and targeting certain proteins moieties against SARS CoV-2 for the development of methods of safety, efficacy and potential vaccine candidates. Many candidates showed efficacy in In-vitro studies but relatively few clinical studies proceeded through different vaccine development platforms, such as entire virus vaccines, plant-based and nucleic acid vaccines, recombinant protein subunit vaccines. This review study provides a short description of SARS-CoV-2 characteristics and deals with recent developments in the design of attempts to produce vaccines to combat COVID-19.

Emine Sen   Tugce Ogut   Abdullah Olgun   and Ozgul Kisa   

Increasing resistance against classical anthelmintic drugs makes discovering new anthelmintic compounds from natural plants important. Nigella sativa (N. sativa) is used as a medicinal plant overall the world and is known to have anthelmintic activity. Caenorhabditis elegans (C. elegans), a common cost-effective model organism that is easily maintained, is useful to determine the anthelmintic activity of new compounds derived from natural products. In our study we aimed to evaluate through toxicity assays the nematocidal activity of N. sativa on C. elegans during its larval and adult stages. Different concentrations of N. sativa oil (900, 450 and 270 mg/mL) were tested and toxicity assessments were done under stereomicroscope by counting the number of surviving nematodes. This study showed that N. sativa essential oil significantly decreases survival of C. elegans in both larval and adult stages at 900 mg/mL final concentration. Larval-stage worms were more sensitive to N. sativa essential oil than were adults. We recommend further studies on other effects of N. sativa on C. elegans after removing the toxic compound(s) from the extract. The further discovery of N. sativa essential oil compounds responsible for anthelmintic activity and determination of their mechanisms of toxicity can pave the way toward new medicines.

Mikhail Gorbachev   

This paper discusses the landmark anthelminthic substances – traditional medicine components, different categories of pluripotential synthetic and naturally occurring compounds. Much attention is paid to the sections devoted to recent discoveries (Emodepside, Monepantel, Derquantel, Tribendimidine) and to some promising works. This review focused on some aspects of molecular mechanisms of action of anthelminthic substances and of helminth adaptation to anthelminthic substances, and on alternative worming treatment options. A new substance development, be it designing a new compound or identification of properties of any existing compounds, is a time-consuming and expensive process. Application of the diversification (different types of compounds) and the focused (related compounds) screenings, software-based evaluation of anthelminthic activity in silico, chemical and genetic trials on model small animals (nematodes Artemia salina, Caenorhabditis elegans, etc.) are intended to accelerate introduction of new substances. Further knowledge in molecular action mechanisms of anthelminthic agents and in resistance development would improve planning of helminthoses control protocols. Based on the systemic analysis of particular features of the chemical structure of anthelminthic substances, the hypothesis on the viability of the targeted search for such compounds among the derivatives of conditionally progenitor cyclic hydrocarbons – benzene, indene, naphthalene, 1Н-cyclopenth [a]-naphthalene, anthracene and phenanthrene – by alternating absolutely unsaturated and saturated structures, including heterocyclic analogues containing nitrogen, oxygen and sulfur and different substitutes and functional groups, was voiced.

Rahul Krishna Puvvada   Krishna Undela   Samaksha P B   Ann V Kuruvilla   and Balaji Sathyanarayana Gupta   

Pharmacy Practice students play an important role in identifying and reporting Adverse Drug Reactions (ADRs). Prior studies focused on knowledge of pharmacy students on reporting ADRs. There are no studies conducted to assess the knowledge and understand the perception of students on causality assessment of ADRs. A web-based cross-sectional study was conducted from October 2019 to April 2020 among the Pharmacy Practice students in various pharmacy colleges across India. Consent form was obtained before filling the questionnaire. The questionnaire was distributed through social media applications and staff of respective colleges. Descriptive analysis was performed to calculate frequencies and percentages of categorical variables. A total of 723 students, 608 responses were received from 30 pharmacy colleges across India. The mean age (SD) of participants was 22.95 (1.61) years. The majority of responses were received from females (70.39). The majority of participants (90.78%) were aware of various causality assessment scales. More than half (58.55%) strongly agreed that there is a need for hands on training on causality assessment of ADRs at college level. Around 80% of the participants strongly agreed that clinical pharmacist is necessary in the healthcare team for causality assessment of ADRs. The knowledge of students on causality assessment of ADRs was found satisfactory. Students believed that having regular workshop on causality assessment of ADRs may help improve their skills in identifying the suspected medications that caused ADRs and helps in better patient care.

Balakrishna Vuyyala   D Senthil Kumar   and Thakkalapally Lakshmi   

Background: Cajanus cajan is a legume of the plant family Fabaceae. Another name of this plant is the red gram, gungo pea, and no-eye pea. It is a multifaceted plant as it is widely often consumed as a dal. It contains wealthy proteins. The whole plant parts are utilized for silkworms as a vegetable; tops, green leaf, and husk are utilized as feed. Objective: The objective of the analysis was to determine the anti-anxiety effect of varied extracts viz n-hexane, chloroform, ethyl acetate, and methanol of the leaves of Cajanus cajan with an EPM (Elevated plus maze) as well as actophotometer model in albino mice. Methods: In the present research, the anti-anxiety activities of several extracts were evaluated viz n-hexane, chloroform, ethyl acetate, & methanol of the leaves of Cajanus cajan with an EPM model in albino mice. Albino mice have ministered with varied extract dosages orally (for example, 200 & 400 mg/kg) and behaviour on the EPM has been seen. The standard usage of Diazepam (2 mg/kg P.O.) (positive control). Results: Results indicate that the methanolic extract of C. cajan manifested a significant as well as maximum dose-dependent impact at 200 & 400 mg/kg on mice with the help of the EPM model and the results were exactly like diazepam (2 mg/kg), the standard antianxiety substance. The model actophotometer exhibited a dose-dependent reduction in locomotor activity compared to control animals, which is shown at two distinct dosages (200 & 400 mg/kg) of Cajanus cajan. Conclusion: The content of polyphenols was shown in the phytochemical test for methanol extract, which could be liable for the anxiolytic potential of Cajanus cajan. This plant might thus also be cultivated as a potentially beneficial anti-anxiety substance.

Namitha R.   G. Sathya Priyadarshini   and Selvi G.   

Pharmacological importance of the nitrogen heterocycles is countless. The triazines are found to possess exceptional biological antitumor, anti-HIV, antiviral, antimalarial, antimicrobial, cytotoxic activities. The current investigation attempts to evaluate invitro antibacterial, antifungal, antioxidant potential, and cytotoxicity of newly synthesized substituted 4'-methyl-3-thioxo-1,2,4-triazinoquinolin-5-one. The antimicrobial activity was done by Agar Well Diffusion Method and the MIC of the compound was found using the Broth dilution assay method. The compounds showed excellent antibacterial activity against selected bacterial strains, including Gram-positive S. aureus, S. pyogens, and Gram-negative bacteria P. aeroginosa, E. coli, K. peumoniae, Pseudomonas Sp with the zones of inhibition 9 to 19nm. The standard drug Ampicillin showed a maximum inhibitory zone 18 nm. Among all the screened compounds, sample exhibited good activity. Similarly, the compounds were screened for antifungal properties, which showed an excellent reduction in the growth of selected fungal strain for Candida albicans. The compounds were also screened for 1,1-diphenyl-2-picrylhydrazyl (DPPH) activity. Cytotoxicity was done in Dalton's Lymphoma Ascites (DLA) cells which were obtained from Amala Cancer Research Center. The tested compounds exhibited significant antioxidant activity in a concentration-dependent manner.

Deepthi Yada   T. Sivakkumar   and Nimmagadda Srinivas   

Inflammation is characterized as a local reaction to the injury of any agent by living mammalian tissue. This is a body defense reaction for eliminating or reducing the spread of the damaging agent, followed by removal of the cells and tissues of necroses. Aqueous extract of Hyptis suaveolens whole plant has been evaluated for anti-inflammatory activity on albino wistar rats by computing the carrageenan-induced paw edema suppression formed by 500mg/kg and 250mg/kg aqueous extracts. Lower dose (250 mg/kg) also suppresses edema formation significantly, when compared to control but unable to reach significant level as 500 mg/kg extract. Indomethacin suppresses the edema formation significantly when compared to the control. Indomethacin has been used as the standard drug. Anti-inflammatory effect was further assessed using stair climbing Activity, motility test and Cytokine assay methods. Stair climbing score, motility score was significant in case of 500 mg/kg of plant extract when compared to control. In Cytokine assay, IL-10, IL-6, and TNF-α have been assessed. IL-10, IL- 6, and TNF-α have been reached to near normalcy after treatment with standard (Indomethacin) and Hyptis suaveolens whole plant aqueous extract (250mg/kg and 500mg/kg). The results of the study rationalize the conventional utilization of plants as an anti-inflammatory agent.

Jayalakshmi B   Kavya Yadav P G   Murali M   and Amruthesh K N   

Various reactive species which are either radicals or non radicals formed during normal metabolic processes. Oxidative stress has been identified as a major causative factor in the development and progression of several life threatening diseases, including neurodegenerative and cardiovascular disease, Antioxidants play a vital role in preventing or delaying oxidation and scavenging free radicals. Plants have been used as exogenous antioxidants from several years. In this contest, the rhizome extracts of two important medicinal plants Curcuma amada Roxb and Zingiber officinale Rosc were investigated for antioxidant properties and phytochemical constituents. Antioxidant capacity of different solvent extracts of these plants was estimated by scavenging diphenyl picryl hydrazyl (DPPH), nitric oxide (NO) and hydrogen peroxide. The petroleum ether and alcohol extracts of Curcuma amada showed stronger antioxidant activity with IC₅₀ values of 26-30µg/ml and 25-29µg/ml, respectively in all the methods while methanol extract showed moderate activity, while petroleum ether and ethanol extracts Zingiber officinale reported good scavenging activity in all the three methods with IC₅₀ ranging from 25-30µg/ml except hydroxyl radical scavenging method. Petroleum ether extracts of both the test plants exhibited good inhibition of free radicals generated by DPPH, hydrogen peroxide and nitric oxide when compared to standard ascorbic acid. The phenolic substances are commonly present in all the studied extracts. Among the two medicinal plants tested, Zingiber officinale has better scavenging activity in all the performed methods followed by Curcuma amada. In the present study, potent antioxidant activity of Zingiber officinale and Curcuma amada extracts leads to scientific validation of these plants. A natural substance which is a part of daily diet and nutritional supplement with antioxidant property constitutes a new source of herbal drug.

Ali Yousofi   Kawsar Alami   and Sayed Yousof Mousavi   

The purpose of this study is to evaluate the effect of Afghan Ferula assa-foetida L. and Crocus Sativus L. aqueous extracts either alone or in combination on morphine withdrawal signs. For this purpose, rats were randomly divided into 13 groups (1 Normal, 1 Morphine, 4 Ferula assa-foetida-treated groups, 4 Crocus sativus-treated groups, and 3 combination groups). Morphine dependency was rendered by subcutaneous injection of morphine hydrochloride for 4 days (10, 20 and 40 mg/kg doses twice daily for 3 days and a single dose of 60 mg/kg on 4th day). Various doses of extracts were injected into extract groups simultaneously with morphine. After two hours of last morphine administration, withdrawal signs were induced by naloxone (3 mg/kg) and noted for 30 minutes. According to the results, different doses of Ferula assa-foetida and Crocus sativus extracts and their combination (in low dose) could significantly decrease the number of morphine withdrawal signs (P<0.05). However, the combination of Ferula assa-foetida and Crocus sativus extracts in high doses showed toxic effects. In conclusion, Ferula assa-foetida and Crocus sativus extract combination in low dose can decrease the morphine withdrawal signs, but without any synergic effects.

Nada M. Ali   

Various medicinal plants are found in the dense forest of Albaha region, southwest of Saudi Arabia. These plant species are natively utilized for the prevention and treatment of various diseases. This study was designed to analyze the chemical composition of ethanolic, petroleum ether, chloroform, and methanolic extracts of Rosmarinus officinalis (rosemary) collected from Albaha region and evaluate the antimicrobial and cytotoxic activities of these extracts. Fresh aerial parts of R. officinalis (stem and leaves) were used for extraction. Then the crude extracts were investigated by using gas chromatography- mass spectrometry (GC-MS) technique to determine their chemical constituents. Antimicrobial assays were performed using Bacillus subtilis and Staphylococcus aureus (Gram-positive bacteria), Escherichia coli (Gram-negative bacteria), and Candida albicans (fungus) to determine the antimicrobial activities. MTT assay was applied to MCF-7 (human breast cancer cell line) as well as on HCT-116 (human colon cancer cell line) to calculate the IC₅₀ of different plant extracts. The GC-MS analysis showed that only petroleum ether extract has an abundance of cyclohexane compounds including 46.5% methyl-cyclohexane. Significant antibacterial and antifungal actions against the tested strains were shown by the petroleum ether and chloroform extracts in antimicrobial assay. Antibacterial activity against S. aureus (SA) and E. coli (EC) was exhibited by methanolic extract, whereas no effect was observed on B. subtilis (BS) and C. albicans (CA). In MTT assay, the petroleum ether extract showed the greatest cytotoxic activity against MCF-7 (3.77 ÎĽg/mL) and HCT-116 (3.09 ÎĽg/mL) cells. The extract of chloroform also displayed significant cytotoxic effect but only against MCF-7 with IC₅₀ values of 12.7 µg/mL. The present study showed that the R. officinalis petroleum ether extract contains significant antimicrobial and cytotoxic activities which can be accredited to the plentiful manifestation of methyl-cyclohexane, methylbenzene and other cyclohexane derivatives, and it may be used to develop new antimicrobial and anticancer drugs.

Iizhar Ahmed Syed   Chandrasekhar Patro   Asim Muhammed Alshanberi   and Shakeel Ahmed Ansari   

The present study involves the formulation and characterization of valsartan (VT) oral disintegrating tablets by using crospovidone (CP) and Hibiscus rosasinensis (HRS) mucilage as complexing agent. Valsartan (VT), anti-hypertensive drug (class II) is an orally active non-peptide triazole-derived antagonist of angiotensin II. The direct compression method was used to obtain 13 such formulations, and the tablets obtained were evaluated for drug content, hardness, friability (FT), disintegration time (DT) and dissolution rate. A significant increase in the dissolution rate of VT was obtained. FTIR and DSC studies showed no interaction between the drug and excipients. The amount of CP (X₁) and amount to HRS mucilage (X₂) is selected for 3² factorial designs. The DT (Y₁), FT (Y₂) and % drug released at 25 min (Y₃) interval were taken as the response variables. X₁ and X₂ represents the result of changing the variable at a time from low level to high level. The interaction terms (X₁X₂, X₁², X₂², X₁²X₂ and X₁X₂²) exhibited that Y₁, Y₂ and Y₃ had changed simultaneously (as analyzed by Design expert software 8 version). The contour and 3D plots revealed that there is an effect of X₁ and X₂ with the interaction on Y₁, Y₂ and Y₃. F₂ formulation exhibited minimum errors with CP and HRS in response to dependable variables which is concluded as best formulation.

Udodi Princewill Sopuluchukwu   and Ezejindu Damian Nnabuihe   

Flunitrazepam (Rohypnol) is a benzodiazepine drug medically proscribed in United States whereas it's legally prescribed in over sixty nations where the drug is administered as pre-anesthetic drug and in the treatment of insomnia but not without the loss of cerebral cortex functions which inspired this investigation to establish its neurotoxicity on the cerebral cortex of adult wistar rat. Sixteen adult female wistar rats were randomly divided into four groups with four rats in each group (A, B, C and D). Group A, the control group received distilled water. Groups B, C and D received 1mg/kg, 2mg/kg and 3mg/kg of Flunitrazepam (Rohypnol) respectively. The animals were sacrificed after three weeks of administration and the cerebral cortexes were harvested and fixed in 10% formal saline for histological processing and studies. The anthropometric investigation presented an insignificant increase in the relative body weight of the test groups when compared to the control group and also presented a significant increase in the relative organ weight in the entire test groups when compared to the control group. The cerebral cortex of experimental animals showed; severe lymphocytic infiltration, focal areas of liquefactive necrosis, intracerebral hemorrhage, vacuolation and various degrees of damages to the tissue layers and neuronal cells of the cerebral cortex. This scientific investigation indicates that consumption of Flunitrazepam (Rohypnol) across various graded doses causes changes in the cerebral cortex histoarchitecture which explains the rationale behind the loss of cerebral cortex function in drug addicts and patients placed on prolonged Flunitrazepam (Rohypnol) therapy.

Mohit Shakya   Shivani Raizada   Rajesh Yadav   and Pratichi Singh   

Acid phosphatase 5 (ACP5) gene plays a vibrant role in the synthesis of a tartrate-resistant acid phosphatase (TRAP5) enzyme. TRAP5 is ~35 KD glycosylated di-iron metalloenzyme responsible for the regulation of osteopontin (protein) activity. There are two isoforms of TRAP5, TRAP5a, and TRAP5b. TRAP5a functions with low enzymatic activity due to a loop interacting with the active site and the more active TRAP5b is generated upon proteolytic cleavage of this loop. TRAP5a works as a marker for systematic macrophage function and chronic inflammation activity, while TRAP5b for osteoclast activity. ACP5 is evolutionarily conserved in nature and acts as a multifunctional protein that involves generations of reactive oxygen species, normal bone development, macrophage function, and osteoblast regulation, affecting a series of pathways, as well as reflecting bone resorption and osteoclast activity. To understand its fundamental role, a functional investigation of missense mutations of the ACP5 gene was carried out through an in-silico approach. Two nsSNPs G109R and L201P were predicted to be deleterious using multiple computational tools like SIFT, Polyphen-1, PolyPhen-2, MAPP, SNAP, Predict SNP and PhD-SNP. Additionally, the structural analysis was performed. The result is that there was no similarity between the native and mutant structures. Therefore, these reported mutations in ACP5 modify the expression, function, and structure of a TRAP5 protein. These findings suggest that TRAP5 can be a therapeutic target in immunological disorders, cancer, and metabolic bone diseases. These deleterious mutations can be lethal to its function and may hamper its therapeutic strategy leading to various diseases such as autoimmune cytopenia, systemic lupus erythematosus (SLE) immune-osseous dysplasia, spasticity with leukodystrophy, moyamoya syndrome, and sjogren's syndrome.

Aliasghar Manouchehri   Pardis Ghanadi   Mostafa Cheraghi   Fatemeh MehrabiRad   Fakher Biglaryan   Mehrnoosh Sedighi   and Leila Mahmoodnia   

Dialysis itself increases oxidative stress. The causes of oxidative stress in patients are not yet known, but uremic toxins, dialyzer interactions, and dialysis fluid contamination have been suggested as three major causes of the stress. Peripheral blood cell-dialysis membrane interaction is another hypothesis that has been proposed for increase in the production of reactive oxidant species. Antioxidants can improve or prevent disease by affecting the involved factors. This article aims to introduce antioxidants that affect injuries due to hemodialysis to familiarize the readers with the disease and prevent and treat the disease using antioxidants. For this purpose, the important effects of medicinal plants with antioxidant properties on the levels of production of reactive oxygen species (ROS), nitrogen (NO), peroxynitric acid, protein oxidation, lipid peroxidation and reduced malondialdehyde (MDA) production and apoptosis in dialysis were investigated and reported. To conduct this review, relevant articles retrieved from Pubmed, ISI and Scopus databases using search terms antioxidant, reactive oxygen species (ROS), dialysis, and kidney, and indexed from 1991 to 2019 were used. Herbal active ingredients such as phenolic compounds, flavonoids and antioxidant compounds can contribute to reducing. It also prevents hemodialysis incidence and its adverse effects by preventing increase of free radicals, decrease of membrane lipid peroxidation, and increase of antioxidant enzymes catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPX). Free radicals affect fat, protein, DNA and cell membranes, including membrane carbohydrates, causing membrane damage and cell disintegration. In terms of clinical applications, antioxidant products can be used to treat oxidative stress related to dialysis and are practical drugs. In addition, small proteins such as immunoglobulin G and complements attach to the membrane of the dialysis machine which activate granulocytes and produce free radicals. Antioxidants with prevent of kidney damage and progression of the disease by affecting the factors effective on hemodialysis.

Haleshappa R.   Sharangouda J. Patil   and Siddalinga Murthy K. R.   

Traditional Indian medicinal plant Simarouba glauca is a highly sacred plant known as "Paradise Tree or Lakshmi Taru" which is recognized for its pharmacological and pharmaceutical properties. The present study was envisaged to know the in vitro phytochemical, antioxidant and free radical scavenging activity of S. glauca seeds. Petroleum ether was used as a solvent to extract plant material using hot extraction method. In our investigation, phytochemical analysis was carried out qualitatively and quantitatively and for the evaluation of antioxidant profile carried out in vitro studies on free radical scavenging potential by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) scavenging, decolourization potential of 2,2'-azino-bis[3-ethyl benzthiazoline-6-sulfonic acid (ABTS) and ferric reducing antioxidant potential (FRAP) assay were determined in in vitro studies. The qualitative phytochemical analysis of this plant was positive for flavonoids, fatty acids, proteins, steroids and terpenoids and in quantitative analysis total flavonoid content was 17.32±0.12 mg/μg quercetin equivalent, total proanthocyanidin content exhibited 62.91±0.61 µg catechin equivalent, total phenol content exhibited 17.75±5.82 μg gallic acid equivalent and the total flavonol content was 1.54±0.01 µg quercetin equivalent of the extract. In the antioxidant profile, the maximum DPPH scavenging activity exhibited was 74% with an IC50 value 137.89 µg/mL, the maximum ABTS scavenging activity exhibited was 35% with an IC50 value 337.29 µg/mL and FRAP scavenging activity exhibited 62.5 µg/mL as ascorbic acid equivalents (AAE/ml) concentration. These findings evidenced that, the petroleum ether extract of S. glauca seeds has potential source of natural antioxidants and can be used it as therapeutic medicine.

Abdul Hafeez   and Shmmon Ahmad   

Quality of pharma-services is defined by the strategies of the pharmacy practices & the patient outcomes. In order to prevent the disease & provide the drug therapy to patients, the strategies of pharmacy practices should be enhanced accordingly. The main aim of the pharmacists' professionals is to enhance the quality of the health-care services by adopting the favourable practices. The standards of the services mainly depend upon the provision of the service. Hence, the aim of present research is to identify qualified pharma-service by adopting the service delivery model for community pharmacy. Previously, the pharmacy practices and the standards were described in several ways, for example, analysing the quantitative aspects related with the pharmacy practices, depending upon the strategies of pharmacy practices that allows personal or indirect use of their advanced healthcare expertise, for patients or other healthcare professionals, to improve the treatment cycle with a view to enhancing healthcare outcomes and importance of healthcare. The interpretation of qualified pharmaceutical services integrates operational function principles, method metrics and result steps. A basic computational framework is introduced to integrate all community pharmacy programs. The term can assist in multiple ways including awareness of the broad spectrum of facilities offered by pharma-community, & promoting establishment of benchmarks for the development and effective delivery of qualified pharmacy services.

Ashok Kumar   and Satish Kumar Sharma   

The term "genetically modified organisms (GMO)" is becoming a contentious issue as its advantages both Potential biomedical impacts and side impact on the economy are bolstered for food suppliers and users. GM animal feed is an emergent method that may affect livestock as well as the pharmaceutical industry. Whilst two pharmaceuticals have yet to join the industry, food materials derived from GE animals. In order to revisit the progress in identifying the main causes, the study was carried out. Affecting GM applications adoption and their possible risks and advantages, GM-derived food products have still not entered the market. However, the active conversation on GM crops and the current conversations on a basis with socio-economic concerns involving the incorporation with GM animals through food and pharmaceutical chains lay the protection and values of food and medicinal products derived from the cloned animals. The same key influences driving the introduction of genetically modified animal products in agriculture including pharmaceutical chains were its endorsement by the population and farmers, government decisions, human wellbeing, animal welfare, impact on environment and conservation. Throughout this paper we explored the financial and leadership benefits and drawbacks of genetically modified animal or pharmaceutical products, and their effect on their introduction.

Samera Ali Siddique   

A collective pharmacy is a recognized concept, authorized and licensed based on the laws and regulations of particular countries. This organizational structure provides the power, control, and enablers for the treatment cycle and includes administrative processes, services, staff, and equipment. Such elements may be helpful when evaluating a company. To define a company as a qualified pharmacy operation, it should be taken in or arranged by a pharmacy and conducted on or offsite. The patients' treatment outcome depends upon the pharmacy practices of the procedures by collaborating with the health-care professionals or the Doctors. 4 major aspects of the medical treatment procedure include an individual access in the drug intervention, pharmaceutical medical programs, strategies regarding the pharmacy procedures and analysis of the obtained results. The method will be applied through laboratory environments, taught in advanced degree courses, incorporated into the clinical rotations of the candidates, developed through internship training & utilized in the form of a model for potential research for evaluation of medical professionals' impact upon consequences related to Medication for patients. Various reports have been evaluated which are relevant to medicinal pharmaceutical programs, although it is challenging to establish which patient treatment procedure has been included in each of these researches.

Ahmed Ibrahim Fathelrahman   

The general aim of the present study was to assess the readiness of pharmacists from a low-income country to counsel patients about medical devices. This cross-sectional study was conducted among Sudanese pharmacists using a convenience sampling technique. An online survey was used to collect data using Google forms. The survey link was distributed to pharmacists using social media. The main outcomes were awareness, sources of information, self-rating of ability to use, and self-rating of confidence to counsel patients about medical devices. In total, 130 pharmacists responded to the online survey. Most respondents were aged 25–54 years (87.8%), and the proportion of males (53.8%) was slightly higher. Overall, the study revealed an acceptable level of preparedness to counsel patients about medical devices with better preparedness for some devices and less preparedness concerning others such as respirometers and implanted devices. Thermometers, weighing scales, syringes, and blood glucose and blood pressure monitors were reported as the most commonly used devices by pharmacists for their own treatment and were top-ranked in terms of their ability to be used and in terms of confidence to counsel patients. In conclusion, the Sudanese pharmacists surveyed in this study reported an acceptable readiness to counsel patients on medical devices. Overseas, board-certified pharmacists and those who received clinical training showed significantly better preparedness than other respondents.

Shreya Parmar   Arun Kumar   and Rudra Pratap Singh Chauhan   

Arsenic in the present times has caused lots of health hazards to humans. In developing countries like Bangladesh and India the high prevalence of contamination, the isolation and poverty of the rural population, and the high cost and complexity of arsenic removal systems have imposed a programmatic and policy challenge on an unprecedented scale. Although in India, arsenic poisoning in ground water in Gangetic belt especially the districts adjoining the river Ganges right from Eastern Uttar Pradesh, Bihar to West Bengal. These regions are the problem of concern as due to which major health related problems are arising. To combat the present problem, a pre-clinical study was carried out on Charles foster rats. They were treated with Sodium arsenite at the dose of 8 mg per kg body weight for 16 weeks to make arsenic model and upon these arsenic pre-treated rats seed extracts of Piper nigrum at the dose of 50 mg per kg body weight was administered for 4 weeks to study the antidote effects of this plant extract. The Piper nigrum extract not only eliminated the effects of arsenic but also reversed the normal physiological activity in the animal by normalising the activity of liver and kidney. The present study concludes that this novel plant extract possesses hepato-protective as well as nephro-protective activity against arsenic induced toxicity.

Omale S.   Aguiyi JC.   Bukar BB.   Ede SO.   Amagon KI.   Amagon L.   Usman O.   Chinello V.   and Oshibanjo DO.   

Mushrooms, which possess medicinal properties, are also considered a good source of food and basic nutrients. Diabetic patients now use edible mushrooms as a source of low-calorie food. Mushrooms are used to treat and prevent diseases such as diabetes, obesity, heart disease, hyperacidity, cancer, hypertension and also act as immune modulators. In this study, the antidiabetic and antioxidant effects of the fruiting body of Pleurotus ostreatus (PO) in sucrose-induced type-2 diabetic Drosophila melanogaster was investigated. The fresh fruiting body of PO was obtained from the mushroom farm of the Africa Centre of Excellence in Phytomedicine Research and Development (ACEPRD) and dried with the aid of the ASPRE dryer. The aqueous extract of the dried powder was used for the anti-diabetic and survival assay. The fly homogenate was evaluated for circulating glucose, total thiol, acetylcholinesterase, catalase and glutathione-S-transferase. PO was observed to prolong D. melanogaster’s survival time as more flies (> 50%) survived on the extract compared to control (47%), after 28 days. There was a significant (P < 0.05) decrease in the circulating glucose of the treated flies compared with those that were untreated; while no statistical (P > 0.05) difference was observed between the metformin and PO treated groups. In the antioxidant study, an insignificant (P > 0.05) difference between the untreated and treated groups was observed. Catalase activity showed a significant (P < 0.05) difference between the diabetic untreated and PO treated groups. We conclude that the fruiting body of P. ostreatus possessed potent hypoglycemic activities in D. melanogaster induced type-2 diabetes, possibly linked to its antioxidant property.

Laraib Ghazi   Muddassir Shabbir Khanzada   Anum Munir   Sajid Khan   Muhammad Rizwan   and Azhar Mehmood   

Ischemic heart disease (IHD) or coronary artery disease (CAD) is one of the largest death-causing reasons in developing countries. Approximately, every year 15 million deaths due to IHD are reported worldwide. PLG (Plasminogen), PCSK9 (Proprotein Convertase Subtilisin/Kexin type 9), CXCL12 (C-X-C Motif Chemokine Ligand 12), and EDNRA (Endothelin Receptor type A) genes were selected for the study due to their higher rate of mutations in IHD. Drugs that are being used to cure IHD were reformulated by structurally modifying them for repurposing. Reformulated drugs were further analyzed for side effects, toxicity, and ADMET (Absorption, Distribution, Metabolism, Excreation, Toxicity) properties. Molecular docking studies of reformulated drugs with selected genes were performed to determine their efficacy to cure IHD. Interacting amino acid residues in the docked complex of aspirin were identified as Aspartic acid, Arginine, Tyrosine, Proline, Valine, Alanine, Threonine, Iso Leusine, Lysine, Triptophan, Aspargine, Histadine, Cystine. Similarly, for isoxsuprine the residues were Valine, Aspargine, Leucine, Argining, Iso Leucine, Glutamic acid, Lysine, Glycine, Proline, Threonine, Aspartic acid, Histadine and Arginine. In reformulated compounds, the addition of sulfur in the aspirin compound reduced the toxicity from class 3 to class 5 and in isoxsuprine, the addition of nitrogen hydrogen bond in the second aromatic ring reduced its toxicity from class 3 to class 4. It is suggested that both aspirin and isoxsuprine analogs are more effective having least predicted side effects and toxicities than already existing aspirin and isoxsuprine. In the future, these drugs can be used as potential drugs for the treatment of IHD than original drugs because of their low toxicity and side effects. This study can be validated in vitro to confirm its efficacy.

Mahdeb N   Bettihi S   Ghedjati N   and Bouzidi A   

The Peganum harmala, commonly known as syrian street, belongs to the family Zygophyllaceae. Peganum harmala L is widely used in traditional medicine and pharmacology. The evaluation of toxic properties of Peganum harmala is crucial when considering public health protection because exposure to plant extracts can result in undesirable effects on consumers. Hence, in this study the acute IP toxicity of the total alkaloids of Peganum harmala L seeds was investigated in female rats. The oral dose (60 mg/kg) of tested plant extract was administered to two groups of animals (group I and II) in single dose and third group III is control. The first treated group is sacrificed after 24 hours and the second treated group and control group are sacrificed after 5 days. Throughout the treatment, changes in behavioral pattern, clinical sign and body weight of rats in treatment groups are observed. Also, a significant decrease in relative liver mass and serum biochemical parameters (AST, ALT, PAL, Bil D and Bil T) were observed. An increase in red blood cells, hemoglobin and hematocrit was recorded in group II. Histological examination shows that the seed extract of Peganum harmala L has no remarkable toxic effect on the liver of the treated animals of the second group. The result indicates that the IP administration of the total alkaloids of Peganum harmala L seeds plant did not produce any significant toxic effect in albino rats.

Prabhakar Adake   Kumar Gourav   and Mahalaxmi S Petimani   

Objectives: To evaluate the possible anxiolytic activity of methanolic extract of Adhatoda vasica leaves (MEAVL) in Swiss albino mice. Methods: A total of 60 (n=60) mice were used. They were divided into ten groups of six mice each. The dose of 200, 400 and 600 mg/kg MEAVL were chosen after acute toxicity study. First 5 groups were evaluated by Elevated Plus Maze (EPM) and rest 5 group were evaluated by Light and Dark Arena (LDA) model. First group of mice (control) received 0.05ml/10g of Normal Saline, second group (standard) received 1.0 mg/kg Diazepam, third, fourth and fifth group received 200, 400 and 600 mg/kg of MEAVL respectively. Anti-anxiety effect was evaluated 60 min after the oral drug administration. Results: All the results were expressed in mean ± SD. One way ANOVA followed by Tukey- Kramer multiple comparison tests were used to compare between groups. In EPM model, the numbers of entries in open arm were 3.50±1.64, 13.17±7.44, 7.50±4.63, 3.67±1.86 and 4.67±2.94 respectively noted for 1^st to 5^th groups respectively for Normal Saline, Diazepam, 200, 400 and 600 mg/kg of MEAVL. Similarly in LDA model, the numbers of entries in dark arena were 12.17±1.47, 13.17±2.92, 12.33±3.01, 7.17±1.94 and 10.50±3.08 respectively noted for 6^th to 10^th group. This result clearly showed that MEAVL-400mg/KG has antianxiety property when compared to diazepam as evidenced by increase in the number of entries in dark arena in LDA model with p< 0.05. In EPM, MEAVL showed increase in the time spent in open arm and decrease in the time spent in closed arm, as well as increase in the number of entries in the open arm but it was not statistically significant (p>0.05). Conclusion: The current study has demonstrated an antianxiety effect of MEAVL in a dose of 400mg/kg in LDA model. However, the study plant must be further evaluated to confirm the molecular basis of the antianxiety property so that it can be helpful for the society in the near future because of its antianxiety property.

Akinpelu Lateef Abiola   Adebayo Muritala Ayofe   Aiyelero Oyeronke Medinat   Ogundepo Gbenga Emmanuel   Fajana Akibu   Isede Nwamaka Ruthlyn   Akinbiyi Ireyemi Abisoye   and Sani Abdulrahman Ibrahim   

Aim: Milicia excelsa stem bark is used as sedative and for treating mental illnesses among the Hausa tribe of Northern Nigeria, but there is no scientific rationale for its use. Hence, this study investigated the oral acute toxicity and sedative potential of ethanol stem bark extract, n-hexane, ethylacetate, n-butanol and aqueous fractions of the stem bark extract in mice. The phytoconstituents in the extract and fractions were quantified. Methodology: The acute toxicity of the extract and fractions were investigated using OECD guidelines 425 of 2008. The sedative effects of the extract and fractions were investigated using pentobarbital-, and ketamine-induced sleep tests. Results and discussion: The results obtained showed that the acute toxicity of the extract and fractions were > 5000 mg/kg, suggesting that the extract and fractions may be safe. The extract, n-hexane, ethylacetate and aqueous fractions significantly (p<0.05) reduced sleep latencies, indicative of sedative effects, effective for sleep induction, while the extract and all the fractions significantly (p<0.05) prolonged the sleep durations, suggesting sedative effects, effective for sleep maintenance. Conclusion: This study therefore, concluded that the extract and fractions may be safe. The study further concluded that the sedative effect of the extract and fractions may be due to the abundance of flavonoids in the extract and fractions. Thus, providing scientific rationale for its ethnomedicinal use. However, further study may be warranted to isolate and characterize the sleep promoting bioactive principles as well as carry out GABA binding assay of the isolated compound(s) in ESB and its various fractions.

Iraj Goli Khatir   Fatemeh Jahanian   Nooshin Varedi   Hamed Amini Ahidashti   Seyyed Hosein Montazar   and Seyed Mohammad Hosseininejad   

Background and aim: Epigastric pain episodes are one of the most common complaints of patients referring to the emergency departments worldwide. The purpose of this study was to compare the effects of ranitidine and pantoprazole on epigastric pain in the emergency department. Materials and Methods: This randomized clinical trial (RCT) study was performed on 100 patients (50 patients in each study arm) with epigastric pain complaints referred to emergency department of Imam Khomeini Educational Hospital in Sari in 2017. Patients older than 18 years of age with an epigastric pain with early diagnosis of dyspepsia and a visual acuity score of 20 mm high (VAS) were included. Patients were enrolled in two treatment groups: single venous dose of pantoprazole 40 mg and single dose of ranitidine 50 mg. The pain score was recorded 30 and 60 minutes after the intervention. Results: The findings showed that in the pantoprazole group: 9.4% dyspepsia and 37.5% pancreatitis and 12.5% gastroenteritis and 40.6% asymptomatic. Before the intervention, the pain group had a pain score of 10.8 and 8.16 in the pantoprazole group. There were no differences between the two groups (P = 0.888), but after treatment, significant difference were observed in each of the groups after the use (P<0.001). Also, the comparison of the two groups after treatment showed that there was a significant difference in pain severity between the two treatment groups (P<0.001). Conclusion: The results of this study have revealed that Ranitidine and Pantoprazole effectively improve initial epigastric pain, but ranitidine is more effective.

Zunera Turk   Muhammad Hamza   Anum Munir   Sajid Khan   Muhammad Rizwan   and Azhar Mehmood   

Lung Cancer is a type of serious cancer that causes 1.37 million deaths every year all over the world and accounts for almost 18% of all cancer death. PI3Ks establish a lipid kinase family that is important to integrate disparate dimensions of cell functions including cell survival, vesicular trafficking, proliferation, and cell migration. This is an essential pathway in the oncogenesis and advancement of lung cancer. In preclinical studies, PIK3 inhibitors deliver exploratory antitumor activity. The study was established to realize perception and molecular mechanisms that are crucial for potent inhibitors of PIK3CA. In this research work, mutated proteins of PIK3CA were selected, models of pharmacophore were designed and hit compounds were obtained against reference feature pharmacophore by virtual screening. These hit compounds were then docked with the mutated proteins of PIK3CA. Three important features were shown by Pharmacophores, Hydrogen bond donor (HBD), Hydrogen bond acceptors (HBA) and aromatic rings (AR). Through virtual screening, 8 hit compounds were obtained before docking Lipinski rule of five was applied and the compounds that achieved all properties were docked with mutated proteins of PIK3CA. 3 compounds fulfilled all properties and demonstrated the stability of ligands. It is suggested that these compounds can be used for curing PIK3CA involved in lung cancer and on the basis of shared feature novel compounds can be designed against a mutation in PIK3CA involved in lung cancer.

Muhammad Hamza   Azhar Mahmood   Sajid Khan   Muhammad Rizwan   and Anum Munir   

The p53 is also known as a tumor suppressor gene, involved in a variety of cellular processes and signaling pathways. p53 mutations are involved in almost all kinds of cancers, and several treatments are available for p53 mutations but have a number of limitations. Still, there is a need for better drugs. Computational methods are emerging and beneficial tools to guide and interpret experiments to fasten the drug design process. This study was undertaken to design a drug that targets p53 Ser121 and Val122 mutations. The compound was identified through virtual screening and several drug-like filters were applied. The identified compound is considered to be non-toxic in nature. ADMET properties and pharmacokinetics of the compound also describe the effectiveness of the compound. The results of this study, suggest that this compound can be used to treat p53 mutations and the compound is synthesized successfully in the lab to determine its adequacy and efficacy. Bis-(4-chlorophenyl)methyl-BLAH compound can be used as a strong inhibitor of p53 Ser 121 and Val 122 mutations.

Iqra Iftikhar   Aqsa Khalid   Zainab Bibi   Azhar Mehmood   Muhammad Rizwan   Sajid Khan   and Anum Munir   

Endometrial cancer is the fourth most common cancer in women. It arises from the endometrium and accompanied by the abnormal growth of the cells. Sign and symptoms include pelvic pain and abnormal vaginal bleeding. It has two categories. Type 1 tumors are estrogen-dependent and they have mutations in PTEN, PIK3CA while Type 2 tumors are more sensitive and have mutations in TP53. Overactivation of the signaling pathway (PI3K) results in anti-apoptosis. Here, this study aims to identify Tumor-Specific Antigen for germline mutations in endometrial cancer which can be used as a potential vaccine candidate. The germline mutations data are obtained from cancer gene census of the cosmic database. Genes mutating with crucial role in endometrial cancer are considered. Peptides libraries are generated using peptide design library. Human leukocyte antigen alleles are identified for the peptide library through NetMHC. Binding affinities of alleles with peptide are determined. Linear regression is performed to generate graphs. PTEN, TP53, PIK3CA, KRAS, and CTNNB1 proved to have critical role. About 575 overlapping peptide libraries are generated and each peptide has a length of 18-20 amino acids. Approximately 58 HLAs are identified, having strong interactions with HLAs. Regression analysis shows that the no. of mutations are directly associated with a binding affinity of peptides. From this, we suggest that the identified TSA can be used as personalized peptide vaccines that directly target the mutated genes in endometrial cancer. This research work can be used in the laboratories for further validation.

Seyed Mohammad Hosseininejad   Fatemeh Jahanian   Iraj Goli Khatir   Seyed Hosein Montazer   Farzad Bozorgi   Nazanin Nosrati   and Farshad hasanzadeh Kiabi   

Introduction: Pain is one of the most common reasons that patients visit emergency departments. Morphine has been used extensively in pain management but there is no consensus about the effectiveness of method of administration. The aim of this study was to compare the divided dose vs bolus medication form of morphine sulfate for management of acute pain in traumatic fracture. Methods: we designed a randomized double-blind clinical trial. On basis of inclusion and exclusion criteria, 160 patients with acute traumatic fracture were enrolled to the study and randomly divided into two groups. The first group (bolus group) received 0.1mg/kg morphine and then 0.1mg/kg normal saline every 5 minutes. The second group (titration group) received 0.1mg/kg of morphine in divided doses every 5 minutes. All injections were intravenously. The primary outcome was pain and before of injection, 15 minutes and 60 minutes after injection were recorded. Data were analyzed using SPSS 19. Results: 77 patients included 49 (63.6%) male with mean age of 47.42 ± 13.15 years were in titration group and 83 patients included 47 males (56.6%) with mean age of 52.40 ± 15.62 years were in bolus group. The complication rate was significantly higher in bolus group (75.9% vs 53.2%, P <0.0001). The need to extra morphine injection in bolus and titration group were 62.7% and 28.6%, respectively (P <0.0001). The mean pain score before and at 15 and 60 minutes after injection were 9.56 ± 1.03, 6.61 ± 1.86 and 1.85 ± 1.13 in titration group and 9.76 ± 0.48, 6.53 ± 1.59 and 0.61 ± 0.46 in bolus group, respectively. The pain score was significantly lower in titration group at 60 minutes after injection (P <0.0001). Discussion: The results of this study showed that titration of morphine are a safe and effective method in compared with bolus administration to reducing acute pain in traumatic fracture.

Mohammad M. Billah   Md. A. Rayhan   Syed A. Yousuf   Kashfia Nawrin   Johir Rayhan   and Elmabruk M. Khengari   

Open Field, Hole Cross and EPM are three widely acceptable experimental methods used to evaluate sedative-anxiolytic potential. The theories behind introducing these fields were to challenge the rodents to a novel environment. However, the behavioral changes caused by these environments often get influenced by rodent's identical neurologic conditions. The major challenges faced by the researchers are variations due to first administration against repeated administration, utilizing same rodent for another experiment but in different time or using different rodent for different experiments. Keeping the drawbacks in consideration, the present study undertook a newly modified (OF-HC-EPM) approach to integrate the experimental fields so as to utilize the same rodents with single oral administration for exposure to different fields which had allowed nullifying the risk of individual and time dependent variance. Anxiolytics, atypical antidepressants, selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, tricyclic antidepressants as well as the combined anxiolytics and antidepressants were administered to Swiss Albino Mice and their respective behavioral changes were observed. The new approach proved to be an essential tool for evaluating neuropharmacological potentials.

Md. Lokman Hossain   and Sharmin Sultana   

Background: Mimosa pudica, a common plant of Mimosoideae family has been used as Ayurvedic herbal medicine by Bangladeshi and Chinese to treat several diseases such as hemorrhoids, hair loss, arthritis, dysentery, leprosy, jaundice, leukoderma, asthma, uterine problems. The root and bark of the plant is said to display antimicrobial activity. Hence, gargling with a decoction of the root and bark of Mimosa pudica diluted in water may help to treat toothaches. Aim of the study: The present study was designed to evaluate the presence of phytochemical groups and to investigate the neuropharmacological activity of methanol extract of Mimosa pudica (MEMP). Methodology: The neuropharmacological activity was determined by hole cross and open field test using Swiss Albino mice as experimental animal. Results: Phytochemical analysis of Mimosa pudica extract indicated the presence of tannins, alkaloids, terpenoids and flavonoids. The sample showed dose-dependent sedative activity at the doses of 200 and 400 mg/kg body weight compared to standard drug Diazepam (1 mg/kg body weight). Conclusion: MEMP showed significant sedative activity demonstrating that the extract may be useful in the development of a new sedative and anti-anxiety drug.

Onuorah Samuel   Nwoke John   and Odibo Frederick   

The diversity of fungi in fifteen public hand-pump borehole water in Onueke, Ezza Local Government Area of Ebonyi State, Nigeria was studied during the dry and wet seasons using standard analytical procedures. The total moulds and yeasts counts were 2-8cfu/ml and 1-5cfu/ml respectively during the dry season and 3-12cfu/ml and 1-4cfu/ml respectively during the wet season. More moulds were isolated from the samples during the wet than the dry season while more yeasts were isolated during the dry than the wet season. The fungi were characterized and identified on the basis of their colonial, microscopic, biochemical and molecular characteristics as Candida albicans, Microsporum canis, Aspergillus fumigatus, Geotrichum candidum, Basidiobolus ranarum, Microsporum audouinii, Fonsecaea pedrosoi and Trichosporon cutaneum. More of the boreholes contained Candida albicans than the other isolates during both seasons. Candida albicans occurred most frequently in the water samples during both seasons while Fonsecaea pedrosoi had the lowest frequency of occurrence in the water samples during both seasons. All the isolates were resistant to Griseofulvin while they exhibited varying degree of resistance and sensitivity to the other antifungal agents used. This study indicated that the borehole water samples examined did not comply with the standard established by regulatory bodies for potable water and therefore must be adequately treated before drinking and use for domestic purposes as these fungi have been reported to cause diseases of humans and animals. Boiling, chlorination, sand filtration and exposure to ultraviolet radiation are recommended.

Kumarappan Chidambaram   Kumar Venketesan   Senthilrajan Dharmalingam   Rajinikanth Siddalingam   Thilagam Ellappan   and Subhash Chandra Mandal   

Background: Ichnocarpus frutescens has been used as Ayurvedic herbal medicine by Gond tribes in India to treat several diseases such as diabetes mellitus and Jaundice. The growing incidence of diabetes mellitus and its complications have headed to the search of novel therapeutic approaches engrossed on preventing postprandial hyperglycemia. The practice of carbohydrate breakdown enzyme inhibitors from plant resources might be a potential approach to prevent glucose absorption with the least adverse effects. Aims: The objective of the present investigation was to provide in-vitro evidence for the potential inhibitory activity of polyphenolic extract (PPE) of Ichnocarpus frutescens on amylase and glucosidase enzymes. Methods: the in the vitro inhibitory effect of polyphenolic extract (PPE) of Ichnocarpus frutescens focused on the evaluation of pancreatic amylase inhibition, rat serum amylase inhibition and rat intestinal glucosidase inhibition of polyphenolic extract (PPE) of Ichnocarpus frutescens by in vitro. The different concentrations of polyphenolic extract were subjected to amylase and glucosidase inhibitory assay and the percentage of amylase and glucosidase inhibitory activity and IC₅₀ values were calculated. Results: Polyphenolic extract shows appreciable pancreatic amylase inhibitory activity in vitro. The extract also showed an appreciable glucosidase inhibitory effect in a concentration-dependent manner with a moderate amylase inhibitory activity. The in vitro examination of the inhibitory effect of PPE on maltase and sucrase activities revealed that PPE inhibited rat small intestine disaccharidase (glucosidase) activity. Conclusion: Taken together, these results suggest that inhibitory effect of PPE on amylase and glucosidase activities may delay carbohydrate digestion and absorption with subsequent lowering of blood glucose level leading to prevention of postprandial hyperglycemia in diabetes and its complication.

Akinpelu Lateef Abiola   Adebayo Muritala Ayofe   and Adesola Adedoyin   

Aim: An earlier study has demonstrated the in-vivo antidepressant effect of methanol stem bark extract of Adansonia digitata, using soxhlet extraction protocol, but there is a lack of scientific data on its neurobehavioural mechanism of action. This study, therefore, investigated its antidepressant potentials, using cold maceration method, and determined the probable neurobehavioural mechanism of its antidepressant-like effect. Methodology: The antidepressant-like effect of the extract was evaluated in tail suspension test, at graded doses in mice. Subsequently, the probable neurobehavioural mechanism of the antidepressant-like effect of the extract was investigated by intraperitoneal pretreatment with adrenergic, serotonergic, dopaminergic, and muscarinic cholinergic receptor antagonists; GABA agonist; nitric oxide precursor and inhibitors; and using a putative neuromodulator at NMDA receptors prior to the extract administration. Results and discussion: The extract at all the doses used, significantly (p<0.05) and dose-dependently decreased the immobility time in tail suspension test without significant (p>0.05) alteration on locomotor behaviour in mice. However, the anti-immobility potential of the extract was significantly (p<0.05) reversed by prazosin, yohimbine, sulpiride, methylene blue, L-arginine and baclofen, suggesting the involvement of adrenergic, dopaminergic, GABAerargic and nitergic pathways. Conclusion: This study, therefore, concluded that the extract may possess antidepressant effect and its mechanism may involve multiple pathways.

Md. Jahidul Hasan   Jamia Ahmad   Ahmad Mursel Anam   and Raihan Rabbani   

Adverse drug reaction (ADR) is a serious life-threatening event and toxic epidermal necrolysis (TEN) is a serious ADR where severe skin lesions like, blisters with oral mucosal bleeding (OMB) are most common characteristics. Both watery blisters and OMB are painful conditions in TEN and considered as common source of infections. N-acetylcysteine (NAC) has anti-inflammatory property and the objective of this study was to observe the clinical response of NAC in the TEN-associated lesions management. For this study, we considered 17 patients those were suffering from TEN and admitted in the intensive care unit. Those 17 patients were distributed into 2 groups (A and B), where patients of group-A (n=7) treated with NAC while group-B's patients (n= 10) did not get NAC therapy. As a result, in group-A, 6 (85.71%; n=7) patients were found with complete remission of blisters and OMB progression within the 72 hours with 100% 10-day complete healing rate, whereas 60% patients in group-B (n= 10) required >72 hours for complete remission with 80% 10-day complete healing rate. So, NAC can be an effective therapy for prompt healing of life-threatening TEN-associated severe skin lesions.

N'Guessan-Irie Amenan Geneviève   Zinzendorf Nanga YessĂ©   Djatchi Richmond Anderson   Kablan Landry   Kouakou Sylvain Landry   Aka Agnimou LĂ©on   and Djobo AdjĂ© Wilfried   

Dichrostachys cinerea root bark is used in Ivorian folk to manage asthma attack. As asthma is often accompanied with secondary infections, this study aimed to assess its potential effects of this medicine against microorganisms. An aqueous-alcoholic extract was obtained from Dichrostachys cinerea root bark. The growth of bacteria in the presence of the extract was measured by the method of dilution in microplate. The antiparasitic potent of the extract was determined on cell culture in microplate with determination of the parasitic viability by reading the optical density of wells in optical microscope. The antifungal activity of the extract was measured by the method of dilution in tube. At 200; 100; 50; 25; 12.5; 6.25 and 3.125 mg/mL the extract did not inhibit growth of Staphylococcus aureus, Escherichia coli, Bacillus sp, Pseudomonas aeruginosa and Enterococcus faecalis. IC90 of the plant extract on Trypanosoma brucei brucei, Caenorhabditis elegans and Aspergillus fumigatus was superior to 125 µg/mL and on average 50 µg/mL on Leishmania donovani and Candida albicans. In conclusion, the extract did not exert any significant anti-infective effect towards the studied microorganisms, supposing that Dichrostachys cinerea root bark would be effective only to delete bronchospasm, the main characteristic of asthma attack.

Towhidul Islam   Anawara Begum   and Shahed-Al-Mahmud   

Background: Dioscorea pentaphylla L. a common plant of Dioscorea family commonly called five leaves in Bangladesh. The plant contains the alkaloid, carbohydrate, tannin, gum protein, steroid, glycoside, flavonoids. It is used as an analgesic, anti-inflammatory, and Powder of plant extract given orally in abdominal pain after delivery. The aim of the study: The present study was designed to evaluate chemical constituents and to investigate the antinociceptive activity of methanol extracts of Dioscorea pentaphylla (MEDP). Methods: The antinociceptive activity of MEDP was investigated using heat-induced (hot-plate and tail-immersion test) and chemical-induced (acetic acid, Formalin-induced) nociception models in mice at 200 & 400mg/kg doses. Result: Oral administration of the methanolic extract of leaves of Dioscorea pentaphylla L. (200 & 400 kg/mg) dose-dependently reduced nociceptive response to acute pain in acetic acid induced writhing. For acetic acid-induced writhing test highest inhibition (55.40 %) was found in case of highest dose (400 mg/kg) for leaf extract. Whereas standard drug diclofenac sodium causes (46.93%) writhing inhibition. Formalin-induced nociception test showed the significant effect in (200 and 400 mg/kg) for both dosages. On the other hand, MEDP showed the significant effect in hot plate, tail immersion test, at high dose (400mg/kg). Conclusion: MEDP showed significant antinociceptive activity via a multifactorial mechanism of action, indicating that the extract may be useful in the development of a new analgesic drug.

Altamash J.Momin   and Amogh R. Lotankar   

The continuous increase in total congestive heart failure cases and the economic burden associated with it has led to the overwhelming demand for novel therapies. Quite a few drugs for heart failure have shown some promise in preclinical as well as early-phase clinical trials, but most of them were unsuccessful to show the real benefit in pivotal trials. Ivabradine and sacubitril/ valsartan are the new promising drugs to treat heart failure which has been approved recently by the United States Food and Drug Administration. Moreover, some of the newer agents under research offer the potential for noteworthy progress in addition to these drugs. Furthermore, Gene therapy and Stem cell therapy are the recent advances which are being explored and so far have proven to be useful as evidenced by clinical trials. Apart from synthetic molecules, there are also some natural agents such as L-arginine, Coenzyme Q10 etc. which aids in the management of congestive heart failure. In addition to the pharmacological treatment, non-pharmacological intervention also plays an essential role in management of congestive heart failure. To assess the true effectiveness of these attractive compounds future clinical trials with proper patient selection, optimal clinical endpoints and more appropriate study designs are mandatory.

Prashant Kumar Dhakad   Pramod Kumar Sharma   and Sokindra Kumar   

Capparis decidua has traditionally been recommended as an aphrodisiac agent. Although, it's medicinal use has not been scientifically proved. The present study therefore evaluated the effects of hydroalcoholic extract of C. decidua roots, stem and leaf on sexual behavior in normal male rats. The hydroalcoholic extract of C. decidua was administered (100 mg/kg, 200mg/kg) to different groups of male wistar rats for 28 days. The female rats were brought in estrous phase before the mating in each group of male rats. Standard group was administered sildenafil citrate at 5mg/kg orally for 28 days. Control group was administered only distilled water. All the experimental groups i.e C. decidua 100mg/kg, 200 mg/kg, per se group (only C. decidua 200 mg/kg), standard group(sildenafil citrate 5mg/kg) were compared with the control group for parameters evaluated for sexual behavior study. C. decidua at 100mg/kg, 200 mg/kg, and per se treated groups produced significant arousal of sexual activity in male rats. They significantly increased the frequencies of mount, intromission frequency. The mount latency and intromission latency were significantly reduced but ejaculation latency was prolonged significantly. The results indicated that hydroalcoholic extract of C. decidua enhanced sexual behaviour in male rats. The enhanced sexual behavior in male rats at the doses of 100 and 200 mg/kg body weight may be due to the presence of phytochemicals like alkaloids, saponins, flavonoids as these phytochemicals has role in increasing sexual strength, androgen enhancing, and antioxidant activity.

Jubran K. Hassan   Adheed Khalid Sharrad   and Falah Hassan Sheri   

Background: Diabetes associated with multiple metabolic problems in the body, including bone mineralization remodeling, osteoporosis and increase risk of fracture. Quercetin is natural flavonoids and according to animal studies; it has potent antioxidant, antidiabetic and protective effect against bone loss due to various causes. Objectives: explore effect of quercetin as nutritional supplement administrated orally on some bone mineralization bio-markers such as calcium, vitamin D and osteocalcin in Iraqi diabetic patients. Methods: interventional double-blind placebo randomized controlled study in which 40 patients with type 2 diabetes mellitus (age range 40-45) assigned randomly (using simple randomization) in either control (n=20) or study (n=20) group. Study group received Quercetin oral supplement as 500mg capsule once daily for three months. Venous blood was used for measuring Serum calcium, 25(OH) vitamin D and osteocalcin at base line and after 3 months. Results: After 3 months treatment with Quercetin; levels of Osteocalcin (28.1±7.6), serum calcium (9.2±1.8) and 25(OH) vitamin D (26.6±8.7) were significantly (p<0.05) higher than pretreatment values of osteocalcin (24.0±8.6); serum calcium (7.0±2.2) and 25(OH) vitamin D (20.6±7.7) and control values of serum calcium (6.8±2.0) and 25(OH) vitamin D (20.8±7.4), but not Osteocalcin (25.2±9.0). There was also significant correlation between use of quercetin; elevation of serum calcium and osteocalcin (r= 0.454; p= 0.032), indicating modulation in bone mineralization. Conclusions: Quercetin's use in diabetic patients may elevate Serum level of Calcium; 25(OH) vitamin D and may modulate bone mineralization represented by elevation of osteocalcin.

Onaolapo A Y   and Onaolapo O J   

Schizophrenia is a chronic, debilitating and complex neuropsychiatric disorder which is known to be characterised by impairments in perception of reality, cognition, interpersonal relationships, mood and social/work function; and influenced by genes and the environment. Our understanding of the aetiology of schizophrenia and theories seeking to explain the accompanying changes in brain chemistry and structure has continued to undergo revisions, largely due to new insights from preclinical and clinical research. In this review, we discuss the evolution of our understanding of schizophrenia aetiopathogenesis as it relates to disease phenotype, symptom management and drug discovery. We also examine the important roles played by interactions between brain neurotransmitters and their receptors in disease expression and symptom management; and discuss how newer chapters in the management of the disease are being opened through the development and identification of newer disease-modifying and modulating agents.

Carol Motycka   Eric F. Egelund   and Cameron Thomas   

Objective: As health care providers, it is important to recognize the potential health issues associated with marijuana use and to educate patients appropriately. As with other types of medication, marijuana has drug interactions, side effects, and the potential for toxicity. In addition, as with other substances that are abused, marijuana has the potential for dependence and addiction. The expanding use of marijuana will increase the pharmacist's involvement with marijuana as part of a patient's regimen. The objective of this paper is to educate health care providers on potential counseling points for patients in regards to side effects, drug interactions and other potential adverse effects from marijuana use. Summary: Currently in the United States, 29 states (plus Washington D.C.) have passed laws allowing for the use of medical marijuana. The possession limit and form of marijuana varies by state. It is imperative that pharmacists understand the laws in their state and the overall effects of marijuana. Conclusion: The increased legalization will continue to expand marijuana's use among patients, necessitating health care providers to be well informed regarding marijuana's side effects, drug interactions, and addiction potential.

Figueroa-Valverde Lauro   Hau-Heredia Lenin   GarcĂ­a-Cervera Elodia   LĂłpez-Ramos Maria   DĂ­az-Cedillo Francisco   Pool-GĂłmez Eduardo   Rosas-Nexticapa Marcela   Herrera-Meza Socorro   Mateu-Armand Virginia   Cauich-Carrillo Regina   and Euan-Hau Saidy   

There are studies which indicate that some fluorobenzene derivatives have inotropic activity; nevertheless, the cellular site and mechanism of action at cardiovascular level is very confusing. To clarify these phenomena in this study, a new fluorobenzene derivative was synthesized to evaluate its biological activity on perfusion pressure and left ventricular pressure. The Langendorff technique was used to measure changes on perfusion pressure and coronary resistance in an isolated rat heart model in absence or presence of the fluorobenzene derivative [0.001 nM]. Additionally, to characterize the molecular mechanism involved in the inotropic activity induced by the fluorobenzene derivative was evaluated by measuring left ventricular pressure in absence or presence of following compounds; ouabain, digoxin, levosimendan, cyclopiazonic acid and thapsigargin. The results showed that the fluorobenzene derivative significantly increased the perfusion pressure and coronary resistance in comparison with the control conditions. Additionally, other data indicate that fluorobenzene derivative increase perfusion pressure in a form similar to ouabain and digoxin; however, this effect was different compared with levosimendan. Other results showed that biological activity induced by the fluorobenzene on left ventricular pressure was significantly inhibited by both cyclopiazonic acid [50 mM] and thapsigargin [300 mM]. These data suggest that positive inotropic activity induced by the fluorobenzene on perfusion pressure and left ventricular pressure was via changes of biological activity both Na,K-ATPase and Ca⁺²-ATPase. This phenomenon is a particularly interesting because the positive inotropic activity induced by this fluorobenzene derivative involves a molecular mechanism different in comparison with other positive inotropic drugs.

Mayson H. Alkhatib   May M. Alasmari   and Faiza Abdo   

A combination of two or more chemotherapeutic agents in a nanoparticle is a promising approach to improve the treatment effectiveness and reduce their toxicity. In this study, the formulations of 30mg/kg of gemcitabine (GEM) mixed with 2.5mg/kg of 5-fluorouracil (5-FU), either loaded on a microemulsion (GEM+5'FU-ME) or dissolved in water (GEM+5'FU-Sol), were examined to explore their antitumor activity in mice inoculated with Ehrlich ascites carcinoma (EAC). Eighty mice were split into eight groups (10 mice/group). Group I served as the untreated EAC bearing mice. Groups II-VIII were EAC bearing mice treated with free GEM (GEM-Sol), GEM-loaded-ME (GEM-ME), free 5-FU (5'FU-Sol), 5-FU-loaded-ME (5'FU-ME), GEM+5'FU-Sol, GEM+5'FU-ME and the blank-ME (B-ME), respectively. The hepatotoxicity was identified by determining the serum enzymes, and studying the histological changes of the liver tissues. The z-average diameter and zeta potential of the nanodroplets of GEM+5'FU-ME were 122.1±26.80nm and -4.40±1.76mV, respectively. Results demonstrated that drug-loaded ME formulations have lowered the enzyme levels of ALT, AST and ALP and did not cause damage in the hepatocytes when compared to the drug solution formulations. In conclusion, the combination treatments of GEM and 5-FU in a ME may protect the drugs from degradation in the liver.

Satish Patel   Deependra Singh   Shikha Srivastava   Manju Singh   Kamal Shah   Durgesh Nandini Chauahn   and Nagendra S Chauhan   

The hasty developments in nanotechnology will have intense impact on various areas of therapeutic applications like drugs and bioactive delivery, tissue engineering, and other application. This review mainly emphasized on the nanoparticle systems for delivery of antimicrobial drug. Various antimicrobial agents have been used to kill or inhibit the growth of microbes such as bacteria, fungi and viruses. As the pharmacological actions of these drugs have been well established, feeble delivery and degradation could lead to insufficient therapeutic index and cause side effects. Nanoparticles have many advantages like small and controllable size, large surface area to mass ratio, and functionalizable structure. These properties make the nanoparticles, a suitable delivery system of antimicrobials. Along with this, it also overcomes the limitations intra-additional antimicrobial therapeutics. In last few years, development and fabrication of antimicrobial agent in nanoparticle systems has evolved as an innovative and promising alternative that increases therapeutic effectiveness and overcoming the undesirable side effects. In this chapter, we focused on the current progress and challenges in producing nanoparticle system for antimicrobial drugs delivery for the treatment of microbial diseases.

Koua Kadio Brou Donald   Kouakou Sylvain Landry   Yapo Adou Francis   Yapi Houphouet Felix   N'tamon Amon Diane Marina   Miezan Bile Aka Patrice   and Kouakou Gisèle Siransy   

Crinum species is frequently used for the treatment of nervous disorders such as epilepsy. This study aimed to investigate the anticonvulsant activity of the hydroethanolic extract of the Crinum scillifolium bulbs in chemoconvulsant-induced seizures in mice. The anticonvulsant activity of the extract (25, 50, 100, 200 and 400mg/kg), was investigated in isoniazid (INH)-induced seizures in mice. The hydroethanolic extract protected mice from INH-induced seizures in a dose-dependent manner. 100% of protection was observed when the animals were treated with 200 and 400mg/kg of hydroethanolic extract of Crinum scillifolium. At Dose of 50 and 100mg/kg 83% protection was observed; the onset of convulsion significant was delayed, and no mortality was found of the mice against isoniazid-induced convulsion. Mice pretreated with hydroethanolic extract at the dose of 25mg/kg reduced mortality to 27% and significant delayed the onset of death (p<0.01). In conclusion, Crinum scillifolium was revealed possessing anticonvulsant effects in mice, via the GABAergic neurotransmission.

Prabhakar Adake   Nagpati Prabhakar Bhat   Roopa P Nayak   Hafis TK   Bhagyashree A   and Prajna V Raj   

Objective: To analyze prescription pattern of antihypertensive drugs in patients with hypertension alone and with coexisting diseases. Methodology: A descriptive cross- sectional study was conducted in outpatient department of tertiary care hospital in south India. A total of 286 prescriptions of patients diagnosed to have hypertension with or without coexisting diseases were collected. Details of prescriptions were entered in the preformed pro forma and analyzed. Result: The study included 138 (48.25%) male and 148 (51.75%) female. Out of 286 hypertensives, 122 (42.66%) patients were having co-existing type 2 diabetes mellitus (T2DM). And remaining 164 patients (57.34%) were only hypertensives. Out of 286 patients, 227 (79.31%) patients were on monotherapy, 49 (17.13%) were on dual therapy and remaining 10 patients were on triple anti-hypertensive drugs. Among 150 antihypertensive drugs that are prescribed for hypertensive patients withT2DM, 57 (38%) were calcium channel blocker (CCB), 40 (26.66%) were angiotensin converting enzyme inhibitors (ACEI), 31 (20.66%) were angiotensin receptor blockers (ARB), 13 (8.66%) were diuretics and remaining 9 (6%) were beta blockers. Similarly, among 206 antihypertensive drugs prescribed for hypertension alone patients, 97 (47%) were CCB, 37 (17.96%) were ACEI, 31 (15%) were ARB, 26 (12.62%) were diuretics and remaining 15 (7.28%) were beta blockers. Conclusion: The study has shown that majority of patients were on monotherapy (79.31%) and calcium channel blockers were commonly prescribed for hypertension in patients with or without type 2 diabetes mellitus followed by ACE inhibitors, ARB and beta blockers.

Prasopchai Tonglairoum   Theerasak Rojanarata   Tanasait Ngawhirunpat   Prasert Akkaramongkolporn   Ruchadaporn Kaomongkolgit   and Praneet Opanasopit   

The aim of this study was to develop erythrosine-loaded electrospun polyvinyl pyrrolidone/ hydroxypropyl-β-cyclodextrin (PVP/HPβCD) fiber patches for plaque disclosing. The fiber patches had been fabricated via electrospinning process and were characterized using scanning electron microscope (SEM), Fourier transform infrared spectrophotometry (FT-IR), differential scanning calorimeter (DSC) and powder X-ray diffractometry (PXRD). The fiber patches were then further evaluated for wetting and integration abilities, mechanical properties, loading efficiency, loading capacity and release characteristic. These erythrosine-loaded fiber patches exhibited excellent wetting and disintegration properties and prompt released the erythrosine form the patches after contacted with saliva. These erythrosine-loaded fiber patches could be exploited as a plaque-disclosing material. However, further in vivo studies are needed for the application.

Onaolapo Olakunle James   Olabintan Olusegun Oyewole   and Onaolapo Adejoke Yetunde   

Objective: We assessed the effects of amitriptyline on open-field locomotion, stereotypic behaviours and spatial working-memory in healthy mice. Method: Five groups of mice were administered vehicle (distilled water), scopolamine (2 mg/kg), or one of three doses of amitriptyline (5, 10 and 15 mg/kg) for 21 days. Behaviours were assessed after the first and final dose of treatment. Result: Administration of the first dose of amitriptyline was associated with enhanced open-field horizontal locomotion, rearing and grooming; with repeated administration, there was suppression of horizontal locomotion and rearing. A dose-related decrease in Y-maze and radial-arm maze spatial working-memory was also observed after repeated administration. Compared to scopolamine, amitriptyline was associated with a significant reduction in open-field behaviours, but a significantly-higher spatial working-memory score. Conclusion: Repeated administration of amitriptyline in healthy mice was associated with suppression of locomotion and grooming; working-memory deficits were also observed. However, working-memory task performance is significantly better than the scopolamine group.

Prashant Kumar Dhakad   Pramod Kumar Sharma   and Sokindra Kumar   

Rajasthan state is rich in flora of xerophytic plants. Capparis decidua (Forssk.) Edgew. is a wild bushy plant found in hot arid regions. This plant has wide range of distribution in many parts of India. Ethnobiologically, this plant is useful as its various parts like immature flower buds, semi-mature fruits, young shoots with small leaves are pickled for use as a condiment and traditional people use this plant in treating ailments like digestive diseases, anodyne, sudorific, constipation, gout, cough, flu, dropsy, palsy, asthma, and intestinal worms, lumbago, odontalgia. Capparis decidua (Forssk.) Edgew. contains chemical compounds like alkaloids, flavanoids, terpenoids, phenolic compounds, steroids, vitamins, quarternary ammonium compounds and many more phytoconstituents that are responsible for its medicinal value. Different parts of this plant like seed, root, stem, flowers, fruits and leaves have medicinal importance and has shown numerous pharmacological activities like antimicrobial, antibacterial, antifungal, anti-inflammatory, antioxidant, hepatoprotective, anthelmintic, antidiabetic, antisebum, antihyperlipidemic, antisclerotic, antitermite, antiplaque, analgesic, sedative and anticonvulsant. Economic importance of this plant has tended for harvesting, yield and marketing specifically in Thar Desert. Future potential of this crop is very promising as it is a drought and heat tolerant plant which makes it a good weather forecasting species; also it provides people with food (pickle & vegetable), fodder, wood and fuel. The presence of numerous phytoconstituents makes it a medicinally important crop for treating deadly diseases. This review covers taxonomy, distribution, phytochemicals, and nutritional value, and commercial value, traditional and pharmacological aspects of Capparis decidua (Forssk.) Edgew.

Amogh R. Lotankar   Altamash J. Momin   Shaijesh Wankhede   and Jyoti B. Sharma   

Aims: An experiment was conducted to evaluate the anti-inflammatory effects of ethanolic bark extract of Plumeria obtusa. Material and method: Anti-inflammatory activity was evaluated by using two different animal models namely cotton pellet method and carrageenan induce paw edema in male Wistar rats at a dose of 100,200 and 400 mg/kg respectively. Results: Phytochemical examination of the extract exposed the existence of alkaloids, flavonoids, tannins and terpenoids. The ethanolic extract elicited highly significant (p<0.001) inflammatory activity in a dose dependent manner on cotton pellet method and carrageenan induce paw edema method. This was noticed by prominently decrease of paw volume in carrageenan induce paw edema and marked increase in % inhibition of cotton pellet Granuloma pouch at the dose of 100,200 and 400 mg/kg respectively. Conclusion: The present investigations showed that the ethanolic extract Plumeria obtusa stem bark has potential anti-inflammatory activity when screened on carrageenan-induced paw edema and cotton pellet Granuloma pouch models in rats.

G. Kallswari   S. Mahendran   P. Subalakshmi   T. Shankar   and P. Ponmanickam   

In the present study the Codium sp. polysaccharide was extracted and partially purified in DEAE cellulose. The polysaccharide was estimated for carbohydrate, sulfate content and uronic acid. The elemental analysis of polysaccharides was analyzed for carbon, hydrogen, nitrogen and sulfur. The antibacterial activity of polysaccharide showed maximum 19 mm of inhibition zone against Bacillus cereus and 12 mm of inhibition zone against Xanthomonas sp. Free radical scavenging activity of polysaccharide from Codium sp. was assayed for total antioxidant capacity, reducing power, hydrogen peroxide scavenging activity, DPPH, ABTS, hydroxyl scavenging assay, superoxide anion radical scavenging and nitric oxide. The green seaweed Codium sp. polysaccharide showed rich sources of antibacterial and antioxidant activity.

Hardik V Vaniya   Nishita H Darji   Vikas R Patel   and Devdatta J Gohel   

Aims: The present study was carried out to describe the patterns of prescription and drug use in Ophthalmology outpatients at GG hospital, Jamnagar, Gujarat, India. Methods: Total of 600 patients were included during 3 months duration and average number of drugs per encounter, percentage of drugs prescribed by generic name, percentage of encounters with antibiotics prescribed, percentage of encounters with an injection prescribed, percentage of drugs prescribed from the WHO Essential Drug List 2015, number of fixed dose combinations prescribed and percentage of antimicrobial agents prescribed were analyzed. Results: Prescription analysis showed that the average number of drugs per prescription was 3.20%. Eye drops were the most commonly prescribed (66.8%) dosage form, followed by ointment (18.4%), capsules (8.66%) and tablets (6%). Dosage forms were recorded in 99.2% drugs, information about the frequency of drug administration was present in 96% of the drugs and duration of therapy was recorded in 84.7% of the drugs prescribed. The drug classes that were used most frequently were Antibiotics (45%), Ocular lubricants (24.7%), NSAIDS (17.4%) and Anti-allergy medications (8.1%). Conclusion: Common prescription errors were minimum. However polypharmacy was common.

N. Nemsitsveridze   N. Gorgaslidze   T. Chumburidze   N. Dughashvili   T. Zarkua   and S. Voronovi   

Pharmaceutical care represents the patient-oriented future profession that is focused on identification, eradication and prevention of the problems connected to the drug treatment. The aim of the study was to detect the role of pharmacist in treatment. Thus it was necessary to find out doctors and pharmacists opinion about this topic. The method of the study was anonymous survey, of pharmacists and doctors. 'Pharmaceutical care'' in Tbilisi pharmacies was evaluated. We performed the analysis of the statistical data from the anonymous questionnaires delivered to 30 pharmacists and 30 physicians. Concerning the character of the request, frequently it is connected to the drug selection which is issued without any prescription, according to the 95% (45% often +50% rarely) of the respondents, majority of the patients request the original medicine to be changed with the generic one, which is according to their opinion determined by the high price of the original medicine. On the question about how many patients are advised, 54% of the pharmacists responded that every day from 50-70 patients address them to select drug or give consultation concerning the drug treatment. On the question about how frequently are patients redirected to the doctors, according to the questioning that consists of 50 %, which means that half of the patients' needs consultation of the doctors and pharmacist warn them concerning this issue. For the reason to find the dependence of the doctors on pharmacist's care we made internet survey. 65% of doctors believe that patient care belongs exclusively to the physician and only 35% of responders agreed to share this function with the pharmacist. In conclusion for avoiding misunderstanding between physicians and pharmacists and also for solving other problems detected during this study it is necessary to upgrade the qualification of pharmacists in clinical issues.

Adikwu Elias   Igbans Rejoice Obele   and Brambaifa Nelson   

This experimental study comparatively evaluated the toxicological effects of treatment with tenofovir, rifampicin and tenofovir- rifampicin (TDF-RIF) combination on kidney function and histology of male albino rats. Male albino rats used in this study were divided into five (5) groups A-E of sixteen (16) animals each. Animals in group A, (placebo control) were treated orally with normal saline, group B (solvent control) were treated orally with 0.1% ethanol while groups C-E were treated orally with 80 mg/kg of RIF, 32 mg/kg of TDF and a combination of TDF- RIF for 2-8 weeks respectively. Animals were sacrificed at the end of drug therapy, blood sample was collected, centrifuged and serum extracted for creatinine, urea and, uric acid evaluation. Kidney was harvested, weighed and examined for histopathological changes. Treatment with tenofovir-rifampicin combination had no significant (p<0.05) effect on absolute kidney weight when compared with treatment using individual doses of these drugs. Insignificant (p>0.05) time-dependent increases in serum creatinine, urea and uric acid levels were observed in animals treated with tenofovir-rifampicin combination when compared with treatment using individual doses of these drugs . Acute tubular necrosis, enlarged glomeruli and obliteration of the Bowman's capsule were observed in the kidneys of rats treated with tenofovir, rifampicin and a combination of tenofovir-rifampicin. This result shows that treatment with tenofovir-rifampicin combination in the management of human immunodeficiency virus /tuberculosis (HIV/TB) co-infection may not be associated with synergistic renal toxicity at the dose level used in this study.

Mohammed Hasosah   Mohammed El Mouzan   Omar Saadah   Khalid Al-Saleem   Abdulrahman Al-Hussaini   Ali Al Mehaidib   Badr Al Saleem   Khalid Alquair   and Kevan Jacobson   

Background: Inflammatory bowel disease (IBD), with its 3 subgroups: Crohn's disease (CD), ulcerative colitis (UC), and indeterminate colitis (IC), is a chronic relapsing inflammatory disorder of the gastrointestinal (GI) tract. Medication adherence is particularly problematic in pediatric IBD. To date this has not been studied in the Middle East. Objectives: The aim of this study was to describe the treatment modalities of IBD and to evaluate adherence to treatment in a population-based cohort of Saudi children. Methods: A cross-sectional study was conducted in all regions of Saudi Arabia. All participating centers were asked to provide information on IBD medications and adherence to prescribed therapies. Results: 354 children with IBD were identified from our database. The age at diagnosis ranged from 1to 14 years, with 145 (41%) diagnosed with UC, 195 (55%) with CD and 14 (4%) with IC. The most common drugs therapy used in IBD was corticosteroids in CD and 5-ASA in UC. Patients with UC were treated with 5-ASA significantly more than patients with CD (76% vs. 62%; P= 0.004). In contrast, patients with CD were treated with infliximab significantly more than patients with UC (22% vs. 6%; P= 0.000). Overall, 15.8% of patients were non-adherent with patients with CD demonstrating a higher level of nonadherence, although this was not significantly different from UC patients (11% vs. 3.8%; P>0.05). Poor adherence to specific drugs was reported significantly more in CD than UC patients; mesalamine (p= 0.022), steroids (p= 0.021) and thiopurines (p= 0.006). Conclusion: Poor adherence occurs most frequently in CD patients and with 5-ASA, corticosteroids and thiopurines. These data can be used to help care providers and policy makers such as the Ministry Of Health define and quantify the burden of IBD among children in Saudi Arabia. Further research in IBD is required to determine the reasons for nonadherence/ poor adherence in the pediatric IBD population so that strategies can be devised to reduce it. Key Points: Medication adherence is particularly problematic in pediatric inflammatory bowel disease (IBD). We found that steroids and 5- Amino salicylic acids are the most widely used medications in pediatric IBD patients. Nonadherence occurs most frequently with 5-ASA, steroids and thiopurines in Crohns. These data should help health care providers quantify the burden of IBD among children.

Adikwu Elias   Brambaifa Nelson   Igbans Rejoice Obele   and Odoko J. Onyedenyifa   

This study comparatively investigated the toxicological effects of treatment with efavirenz, isoniazid and efavirenz-isoniazid (EFV- INH) combination on liver function parameters and histology in adult male albino rats. Animals used in this study were divided into five (5) groups A-E of sixteen (16) animals each. Animals in group A (placebo control) were treated with water while animals in group B (solvent control) were treated with arachis oil orally. Animals in groups C-E were treated orally with 15mg/kg of INH, 10mg/kg of EFV and a combination of INH- EFV for 2-8 weeks respectively. At the end of drug therapy, serum was extracted from centrifuged blood sample and evaluated for alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, total and conjugated bilirubin. Animals were sacrificed and liver was harvested weighed and evaluated for histopathological changes. Effects produced by co-treatment with EFV-INH on absolute liver weight, alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, conjugated and total bilirubin were insignificant (p>0.05) when compared with effects produced by treatment with individual doses of EFV and INH. Histopathological evaluation of the liver of animals treated with EFV-INH combination showed vascular congestion, inflammation of parenchyma and hepatocytes degeneration. These results show that co- therapy with EFV-INH in patients with human immunodeficiency virus /tuberculosis co-infection may not be associated with synergistic hepatotoxicity.

Ashley Choi   Annesha White Lovett   Jinhyang Kang   KyungMi Lee   and Lydia Choi   

The aims of the study were to review the literature within the last decade with regard to existing applications to improve non-adherence, quality of life, and to discuss the pros and cons of currently marketed mobile applications. Based on review of a total of 33 articles and reports, hundreds of medication-related applications were shown to be currently available on the market. The findings were categorized based on the pros and cons of the applications. Results revealed that various applications are helpful to facilitate patient adherence, yet the majority of them have similar functions. These functions consist of manual reminder alerts and access to sources for drug information. Limited studies were found related to quality of life. Observational studies that were retrieved focused on physiological factors, such as a decrease in hemoglobin A1c. The target populations for mobile applications included caregivers, the elderly, low literacy patients, low income individuals, and other patients. Current mobile applications have a beneficial impact on patients, caregivers, and health-care providers including pharmacists. Although there were some concerns regarding methods for using mobile applications, such as privacy issues, the majority of previous studies showed positive perspectives on mobile applications. Future research on compatible features is encouraged for improved mobile application use in healthcare.

Afaf H. Al-Nadaf   and Mutasem O. Taha   

Background: Alzheimer's disease (AD) is a degenerative disease of the brain common form of dementia. A variety of therapeutic strategies for modulating the progression or prevention of AD are currently being investigated. The etiology of the disease is characterized by aggregates of amyloid plaques, largely composed of amyloid-β peptide formed from the amyloid precursor protein cleaved by Memapsin 2(Beta-secretase / BACE1). Based on its key role in the β -amyloid cascade, inhibition of Memapsin 2 is widely recognized as one of the most promising therapeutic approaches for the treatment and prevention of AD. However, the development of small molecule, brain penetrant Memapsin 2 inhibitors has been challenging. Method: Molecular docking study using LigandFit Docking and Scoring as well as LibDock Docking functions were performed as a preliminary in-silico screening test for National Cancer Institute (NCI) database using binding pocket of Memapsin. Followed by in-vitro enzyme inhibition assay, High-ranking docked conformers and poses were scored using seven scoring functions. The validation for our docking–scoring procedure was performed through employing the same conditions to dock a well-known Memapsin inhibitor IO2. High ranking compounds were evaluated in vitro using Memapsin fluorescence resonance energy transfer (FRET) assay. Results: The docking simulation resulted in a close model to the crystallographic structure. Five of the important interactions are shared between the co-crystallized ligand and in-silico hits. Virtual screening identified low micromolar inhibitory leads from the NCI list of compounds. The most potent hit exhibited Memapsin IC50 values of 11.1μM in enzymatic assay. Conclusion: We have identified a low micro-molar Memapsin inhibitor with IC50 of 11.1μM. Our results suggest that in silico high-throughput screening approach can serve as useful source to identify new hits which can be used as lead candidate for synthetic modification in order to reach more potent enzyme inhibitors.

Wesam G. Ammari   Zainab Al-Qadhi   Mohammad Khalil   Rabab Tayyem   Samir Qammaz   Ghaleb Oriquat   Iman A. Basheti   and Henry Chrystyn   

Indacaterol is a recent ultra-long-acting inhaled β₂-agonist bronchodilator. The current work validated an in-house developed high performance liquid chromatography (HPLC)-tandem mass spectrometry (MS/MS) bioassay for indacaterol in human plasma. Ethyl acetate was used in a liquid-liquid extraction (LLE) method to extract indacaterol from plasma samples. A 200 ÎĽL of the mobile phase (water-methanol (30:70, v/v)) was used to reconstitute the indacaterol dry extract. A 5 ÎĽL was then eluted on a C18 column at a mobile phase flow of 1 mL/min. Formoterol was the internal standard (IS). The MS/MS was the detector. Method validation followed the International Guidelines. Indacaterol and IS were detected at a mass to charge ratio of 393.3 and 345.2, respectively. Validated calibration curves were linear over 0.075 - 100 ng/mL. Method specificity was established in 8 different plasma batches. No matrix effect was observed. The intra-batch accuracy (precision) percentages for the lower limit of quantitation (LLOQ), Low, Mid and High quality control levels were 113.6 (10.8), 104.7 (9.1), 99.8 (7.6) and 102.2 (8.5), respectively. The inter-batch accuracy, recovery, short-term and long-term stability results were accepted. Validation has confirmed a specific, accurate and precise HPLC-MS/MS coupled with a simple and fast LLE for indacaterol in human plasma.

Kyoko Ueda   Fumio Tsuji   Tomoko Hirata   Kenji Ueda   Masaaki Murai   Hiroyuki Aono   Masanori Takaoka   and Yasuo Matsumura   

Tumor necrosis factor (TNF)-α plays a crucial role in the pathogenesis of ischemia/reperfusion-induced renal injury. We demonstrated recently that the preischemic treatment with resiniferatoxin, a transient receptor potential vanilloid 1 (TRPV1) agonist, attenuates renal TNF-α mRNA expression, and improves ischemia/reperfusion-induced renal injury in rats. In the present study, we investigated effects of treatment with SA13353, a novel orally active TRPV1 agonist, on ischemia/reperfusion-induced renal injury in rats. Ischemic acute kidney injury (AKI) was induced by occlusion of the left renal artery and vein for 45 min followed by reperfusion, 2 weeks after contralateral nephrectomy. Renal function in vehicle-treated AKI rats markedly decreased at 24 h after reperfusion. Treatment with SA13353 (3, 10, and 30 mg/kg, p.o.) 30 min before ischemia dose-dependently attenuated the ischemia/reperfusion-induced renal dysfunction. Histopathological examination of the kidney of AKI rats revealed severe renal damage, which were significantly suppressed by the SA13353 treatment. In renal tissues exposed to ischemia/reperfusion, TNF-α and cytokine-induced neutrophil chemoattractant-1 mRNA expressions were augmented, but these alterations were attenuated by the treatment with SA13353. On the other hand, ischemia/reperfusion-enhanced renal interleukin-10 mRNA expression and its plasma concentration were further augmented by SA13353 treatment. These results demonstrate that the orally active TRPV1 agonist SA13353 prevents the ischemia/reperfusion-induced AKI. This renoprotective effects seem to be closely related to the inhibition of inflammatory response via TRPV1 activation.

Alemayehu Gutasa   Desta Assefa   and Kabaye Kumela   

Background: Malaria is the most serious health problem in the world. In order to reduce malaria prevalence, knowing of the level of community awareness towards malaria prevention as well as community practice towards treatment seeking behavior is important. Objective: The aim of the study is to assess and identify the level of community awareness towards malaria, their practice of treatment seeking behavior and its relation to preventive measure. Methods: A community based cross – sectional study was conducted. Data was collected from a sample size of 283 households using structured questionnaires from January 28/2013 to February 8/2013. The questionnaires contain three parts depending on the information they contain. They include information about socio-demography, knowledge of the respondents towards malaria and its prevention and community practice towards malaria and its treatment. Result: A substantial number of respondents responded as they have reasonable knowledge on malaria (90.1%); including correct association between malaria and mosquito bites (87.2 %), and most people (85.8%) mentioned burning waste material as vector control method and few respondents were bed net owner (7%). Nearly greater than half (55.7%) of respondents stated that they would seek treatment within 24 hrs of onset of malaria at health facilities as their first treatment option. Finally data was presented in tables, figure and chart. Conclusion: The community overall awareness about the symptoms, cause, transmission and prevention measure of malaria was found to be high. Increasing awareness and access to early malaria diagnosis prompt treatment before the disease become complicated and participation in the health education is vital components in terms of malaria knowledge and practice.

Timothy Allen   Ghazaleh Shoja E Razavi MD   and Giridhar M. N. V   

The article discuss about the role of peptide vaccine in Cancer therapy. A peptide vaccine is a type of vaccine in which a peptide of the original pathogen is used to immunize an organism.

M. Abdul Alim Al-Bari   M. Khairul Islam   M. Shakhawat Hasan   Md. Abdullah Al Mamun   and M. Kudrat-E-Zahan   

The use of probiotic Lactobacilli has moved from concept to implement in different applications. The study was carried out to establish the synergistic role of co-cultures of Lactobacillus casei, L. delbrueckii, L. plantarum and L. helveticus in lemon juice (LJ) preservation as well as investigate the inflammatory- and toxicity profiles of biopreserved LJ ingested shigellosis mice. Lactobacilli were cultured individually and cocultured with different combinations. Four strain Lactobacilli had significant preservative activity than any other combinations in both free and microencapsulated Lactobacilli. The four microencapsulated bacteria extended shelf-life of the LJ in about two weeks at 4°C. The free or microencapsulated bacteria were increased acidic pH into LJ. It was evidently proved that microencapsulated cocultures of different strains remained viable over a long period of time and the probiotically fermented juice were potentially inhibiting the pathogenic growth. For inflammatory acute shigellosis, therapies were divided into six groups: LJ only; LJ containing pathogenic bacteria (PB); LJ containing curd, the source of Lactobacilli; LJ containing curd and PB; LJ containing four Lactobacilli LAB1,3,4,6 and LJ containing chemical preservatives (PR, prophyl paraben and methyl paraben 9:1). Lactobacilli preserved LJ were found to be favorably lower inflammatory haematological profiles such as ESR, WBC count and C-reactive protein (CRP) agglutination in acute shigellosis mice. In addition, biopreserved LJ was safe owing to normal ranges of SGPT, SGOT, SALP and AA levels in shigellosis mice. Prospective studies on mechanisms of the probiotic activities might be enable their new medical applications for food preservation and treatment of inflammatory dysentery patients.

Gannu Praveen Kumar   and Pogaku Rajeshwar Rao   

The formulation and evaluation of diclofenac sodium from liposomes, niosomes and nanoemulsion are analyzed. The release profiles of diclofenac sodium were almost similar in all the formulations. It is found that 85% of diclofenac sodium diffused out from the colloidal systems within 8hrs and practically all the drug was released within 12hrs. In addition to this controlled release, the similarity of the release profiles obtained for liposomes, niosomes and nanoemulsion signifies that the internal structure has little role in the release process. The drug released fast and completely from the carriers upon high dilution, but it is slowed down a little when they are not diluted. The maximium amount of diclofenac sodium was released from nano emulsion as well as liposomes after 12 hrs at 1 in 200 dilution where as in niosomes, it was found at 1 in 100 dilution. But surprisingly, the release was decreased upon further dilution. The higher the surfactant content, the higher the globule size of the nanoemulsion. The mean size of the systems was decreased upon increasing dilution. Among all the systems, the mean size of niosomes was decreased upon increasing the dilution up to 1:200. It was finally depicted that the dilution effect on the zeta potential of the systems shifted from negative to positive by adding polysorbate 80. The zeta potential of all the systems was significantly good indicating stable systems.

Hemalatha Bagavatula   Srinivas Lankalapalli   VS Vinai Kumar Tenneti   Naga Malleswara Rao Beeraka   and Bhanu Teja Bulusu   

Itraconazole is a potent triazole antifungal drug which has low solubility at physiological pH conditions. Itraconazole is weakly basic (pKa =3.7) and highly hydrophobic drug. It is categorized as a BCS class II drug. The main objective of the present investigation was to improve the solubility of itraconazole, by preparation of salt forms itraconazole hydrochloride, mesylate and besylate by using addition reaction with hydrochloric acid, methane sulphonic acid and benzene sulphonic acid. Further inclusion complexes of itraconazole were prepared with Captisol (sulfobutyl ether₇ β-cyclodextrin) by using physical mixing, kneading and co-evaporation techniques. The preparations were characterized by using X-ray diffraction, Fourier Transformed Infrared spectroscopy and Nuclear Magnetic Resonance spectroscopy. The solubility of prepared salt was found multifold than the solubility of itraconazole. The dissolution studies exhibited higher percentage drug dissolution from itraconazole complexes than that of the pure drug which can be attributed to the increase in drug solubility provoked by the complexation technique.

Desta Assefa   and Nezif Hussein   

Background: - Highly active antiretroviral therapies are the drugs of HIV/AIDS treatment with no cure. Even though they inhibit viral replication, they may cause a number of adverse effects; which may end with treatment failure and/or regimen changes. Objective: - The study was aimed to determine the reasons for HAART regimen change among HIV/AIDS Patients on first line HAART during 12 months follow up in Fitche Hospital, ART Clinic. Methodology: - Hospital based retrospective study was conducted at Fitche Hospital, ART Clinic from January 28 to February 12, 2013 by reviewing patients' information sheets and physician diagnostic cards. The data was categorized and analyzed manually using calculator for statistical analysis. The results has been interpreted and presented by tables and graphs. Results: - Majority of the patients 29(42.65%) were on D4T/3TC/NVP at the beginning of the Highly Active Antiretroviral Treatment. The main reason for regimen change was toxicity 56(72.73%) followed by, treatment failure 11 (14.23%), new drug available 7(9.09%), co morbidity 2(2.60%), and 1(1.30%) patient refused to took the drug. From all the toxicities reported, lipoatrophy, which accounted for 73.47% of the toxicities, was the most common. Conclusion: - Results shows that majority of patients were initiated D4T/3TC/NVP compared to other regimens. Toxicity appears as the main reason for treatment and regimen change in this study. The other reasons include; treatment failure, new drug available, co morbidity and patient refused to took the drug respectively.

Vivekanand K. Chatap   Prashant L. Patil   and Savita D. Patil   

The design of the present investigation was to prepare furosemide bounded pharmacosomes to enhance solubility and permeability drug by simple reproducible solvent evaporation technique and further investigated. Furosemide bounded pharmacosomes formulation (PMC1 & PMC2) was taken and compared with pure drug by way of enhanced solubility 5.4 fold in the water, 3.33, 4.76 fold in pH 7.4 and pH 5.8 respectively, increases permeability of furosemide bounded pharmacosomes 28.28% when compared with pure drug, drug content showed 94.83, N-octanol/water partition coefficient from 2.33 to 5.15 and in-vitro release profile exhibits excellent sustained drug release properties. Prepared furosemide bounded Pharmacosomes were confirmed from differential scanning calorimetry (DSC), X-ray diffraction (XRD) and FT-IR. The pharmacosomes reported amphiphilic nature may responsible for the improvement of solubility and permeability leads to enhancement of oral bioavailability. From this study it can be concluded that, this formulation strategy becomes important for drug belongs to the BCS class- II & IV.

Quyen Bach   Annesha Lovett   Teresa Pounds   and Pamela Moye   

In 2008, the American Society of Health-System Pharmacists introduced the Pharmacy Practice Model Initiative (PPMI). The goal of this model is to promote pharmacy leaders, better manage resources, and increase focus on patient-centered and team-based care. Few studies have assessed the model’s implementation. PubMed and CINAHL were searched using keywords “pharmacy practice model,” “organizational,” and the MeSH term, “organizational,” from 2008 to 2013. Of the forty-nine findings (articles and summit highlights), two case studies met the inclusion criteria. The first case study involved the University of Minnesota Medical Center, a multi-campus academic medical center. This facility used technology such as pagers for decentralized technicians, computerized provider order entry, and wireless computers on wheels. The implementation teams worked on clinical and distributive functions allowing for consistency in care and improved employee satisfaction. The second case study involved Providence Health & Services, a multihospital system in Washington State and Montana. These facilities used technology such as automated dispensing cabinets, order-image scanners, and automated telephone trees to route calls. The outcome was a positive economic impact with a return on investment of $709,321. An important finding was the lack of research assessing the implementation of the PPMI. Based on positive findings, it is evident that further research is warranted.

Klaus Martin Beckmann   

ADHD is a neurodevelopmental life time high prevalence disorder. Many individuals who suffer from ADHD benefit from treatment. For a significant subgroup of patients with the diagnosis ADHD, medication is important for treatment. Diagnostic criteria however as yet are not pathognomonic. A specific test to diagnose the type of ADHD that responds to medication has so far not been promoted as such. This article postulates that many individuals presenting with ADHD syndrome are likely to benefit from such a test. Here such a test is described.

Paul E. Brumley   Miroslav A. Anguelov   Jason P. Hecht   and Dane Shiltz   

Enoxaparin, a low-molecular-weight-heparin, is being used in hemodialysis patients despite a lack of guideline or manufacturer dose recommendations. Due to enoxaparin’s renal excretion, the possibility of accumulating anti-Xa concentrations in hemodialysis patients using enoxaparin creates a hemorrhagic risk, calling for more research. The objectives of this study are to determine the correlation between treatment dose enoxaparin use and anti-Xa concentrations within the defined therapeutic range in patients receiving chronic, scheduled hemodialysis to determine the degree of change in anti-Xa concentrations in those cases where a concentration was obtained before and after a specific hemodialysis session, and to determine if there is evidence of enoxaparin accumulation over the course of treatment. This was a retrospective cohort study. Patients that were admitted to Indiana University Health facilities in a two-year period were identified from a Cerner query for inclusion eligibility. Inclusion criteria involved patients that received therapeutic dose enoxaparin based on actual body weight on a once daily basis, maintained a scheduled hemodialysis regimen, and had an anti-Xa concentration obtained after at least one enoxaparin dose. Despite lacking statistical significance, the data collected from this study depicts trends which can be utilized to guide future studies. The results of this study suggest that hemodialysis does not effectively remove enoxaparin.

Manal Ihbeasheh   Ikhlas Jarar   and Waleed Sweileh   

Objectives: The objective of this paper was to study antipsychotic medication use in the outpatient psychiatry department in Palestine. Methodology: This is a cross sectional study carried out in Palestine on schizophrenic patients aged between 20 – 65 whose medications have not been changed in the past six months and they did not have an acute attack in the last year. Information regarding antipsychotic medications use was obtained from patients’ medical files; patients’ psychiatric symptoms were evaluated using the Expanded Brief Psychiatric Rating Scale (BPRS-E).Results: More than half (53.1%) of 150 patients were on antipsychotic polypharmacy (APP) with average daily dose of 546.9 ± 254.9 mg chlorpromazine equivalents. The average number (mean ± SD) of medications a patient received was 1.7 ± 0.7. One third of patients on APP regimen received atypical antipsychotic and all of them received at least one conventional antipsychotic. Factors significantly and positively associated with APP were: use of anticholinergic agents (P<0.001), conventional antipsychotics (P<0.001), depot formulations (P<0.001) and prescribing higher doses of antipsychotics (P<0.001). Discussion and Conclusion: Antipsychotic polypharmacy in this study was common. Adherence to international guidelines in the treatment of schizophrenia is recommended.

M.Kh. Dzhafarov  and F.I. Vasilevich  

This review discusses the landmark anthelminthic substances – traditional medicine components, different categories of pluripotential synthetic and naturally occurring compounds. Much attention is paid to the sections devoted to recent discoveries (Emodepside, Monepantel, Derquantel, Tribendimidine) and to some promising works. The review is also focused on some aspects of molecular mechanisms of action of anthelminthic substances and of helminth adaptation to anthelminthic substances, and on alternative worming treatment options. Based on the systemic analysis of particular features of the chemical structure of anthelminthic substances, the hypothesis on the viability of the targeted search for such compounds among the derivatives of conditionally progenitor cyclic hydrocarbons – benzene, indene, naphthalene, 1Н-cyclopenth [a]-naphthalene , anthracene and phenanthrene – by alternating absolutely unsaturated and saturated structures, including heterocyclic analogues containing nitrogen, oxygen and sulfur and different substitutes and functional groups, was voiced.

Ana R. Pinto   Andreia Machado   Elisabete Gonçalves   LuĂ­s Salsas   Tiago Vicente   Maria I. B. Ribeiro   and Isabel C. J. F. Pinto   

During the last century, the pharmacy professionals have significantly being professionalized, the user is a high priority and not just limited to the sale of pharmaceuticals. As such, it is necessary to know the users, their needs and expectations, their opinions and preferences. This transversal study, observational, correlational, aimed to: determine the degree of satisfaction with the attendance in community pharmacies, if there is a relationship between factors of a personal nature (age and gender) and satisfaction, trying to identify which aspects improve in order to increase satisfaction levels. The sample consisted of 525 respondents. Data collection was conducted in the period from October 2012 to January 2013 in four locations in northern Portugal. It was used a questionnaire consisting of three parts: the first contained items of personal characterization, the second consisted of the scale "Pharmacy Services Questionnaire" (FSQ) validated for the Portuguese language, developed by Larson et al. (2002) and the last had questions about the respondents' opinion. The results showed that the degree of satisfaction with the services of community pharmacies was in majority an average to 39 % and good for 46,1% . Having in mind the factor by gender, females showed a higher degree of satisfaction. Regarding the age group, older users had the highest degree of satisfaction. It was concluded that, generally, community pharmacies bring a higher degree of satisfaction in the older and the female users. "How the pharmacy professionals explain possible side effects" and "how the pharmacy professional answers your questions.", are the two aspects that must be improved to achieve a higher degree of satisfaction.

Anand G. Mundhe   Gokul A. Khairnar   and Sadik F. Sayyad   

Within the oral mucosal cavity, the buccal region offers an attractive route of administration for Systemic patches. Venlafaxine were Prepared using HPMC K4M, Pectin, and poly vinyl Pyrrolidone, PG as Plasticizers. FTIR and UV spectroscopic and DSC methods revealed that there is no interaction between Venlafaxine and polymers. The patches were evaluated for their thickness uniformity, folding endurance, Weight Uniformity, content uniformity, Swelling behaviour, tensile strength, Mucoadhesion strength and Surface pH. In vitro release studies of Venlafaxine loaded patches in Phosphate buffer (pH, 6.8) exhibited 98 % drug release in the 8 h. The optimized patch was obtained good in vitro result.

Leidy G. Fernandes   Vânia F. Rodrigues   Maria I. B. Ribeiro   and Isabel C. J. F. Pinto   

Work is a profession, a craft, or an activity in which man produces something central to his life. The job satisfaction is reflected simultaneously on the worker and the functioning of organizations. Workers more satisfied with their work have higher productivity levels, higher subjective well-being and well-being with life in general. Community pharmacy professionals are categorized in three professional categories: pharmacists, pharmacy technicians and technical pharmacy assistants. Work satisfaction was previously associated with gender, age, job category, years of service, remuneration, security concerning the future of the profession, relationships with colleagues and satisfaction with the professional category. The objectives of this study are to evaluate the satisfaction level of community pharmacy professionals and to identify associated factors. These professionals have revealed, in general, a level of moderated satisfaction. There were no significant differences between job satisfaction and gender, age, years of service, professional category and remuneration.

Katie L Axford   and Dane L Shiltz   

Background. Multi-drug resistant bacteria are a growing concern in healthcare. Daptomycin is being used with increasing frequency in the treatment of vancomycin-resistant enterococci (VRE) and methicillin-resistant Staphylococcus aureus (MRSA) bacteremias in hemodialysis (HD) patients. Thrice-weekly dosing of daptomycin in this population would allow for coordination of dosing with common outpatient HD schedules. The aim of this study is to determine if thrice-weekly dosing of daptomycin is equivalent to dosing every 48 hours in patients receiving chronic intermittent hemodialysis. Equivalence will be assessed with regard to microbiological cure, clinical cure, hospital length of stay, and mortality. Methods. All patients with positive blood cultures who received at least one dose of daptomycin between January 1st 2009 and December 31st 2010 at Indiana University Health Methodist and University Hospitals were identified. Adult patients with end-stage renal disease on a stable thrice-weekly hemodialysis regimen, confirmed VRE or MRSA bacteremia, and at least three doses of inpatient daptomycin therapy were enrolled in the study. Results. Twelve patients met criteria for inclusion in this study. Nine received daptomycin every 48 hours for the treatment of bacteremia, and three received daptomycin thrice-weekly after dialysis. There was no difference in time to clearance of blood cultures between the Q48H and thrice-weekly groups (2.11±2.15 days vs. 4.33±4.16 days; p=0.241).Length of hospital stay was not statistically significantly different between the two groups (22.8 days vs. 14.9 days; p=0.065).Conclusions. Thrice-weekly dosing of daptomycin may be effective for the treatment of bacteremia in hemodialysis patients.

Mokale Vinod   Naik Jitendra   Khairnar Gayatri   and Khairnar Gokul   

Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration.Due to repeated administration there may be a chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability & better patient compliance. Methodology: Alginate beads were prepared by ionotropic external gelation technique using CaCl₂ as cross linking agent. Prepared beads were evaluated for % yield, encapsulation efficiency, swelling index in 0.1N HCL and 7.4 phosphate buffer, drug release study, FT-IR, FE-SEM analysis. In order to improve %EE and drug release, pectin, methyl cellulose and locust bean gum were used as co-polymers along with sodium alginate. Result: Yield was found to be in the range of 72.41-96.43. % EE was 47.3% (F1), 71.1% (F5). In pH 7.4, beads showed increase in swelling index as compare to in 0.1 N HCL. Among use of different copolymers, locust bean gum sustained the DTZ release up to 55.98% (F6) in 12 hrs. FT-IR analysis revealed no drug excipient interference. Prepared beads were found to be rough, with cracks and pores on the surface. Conclusion: It was concluded that DTZ could be successfully entrapped and sustained in sodium alginate beads with use of locust bean gum.

Amrita Kumari   Juhi Rao   Jyoti Kumari   Neha Sharma    Pankaj Jain   Vivek Dave   and Swapnil Sharma   

The present study was undertaken to evaluate the analgesic activity of aqueous extract of Citrullus lanatus peels (AECL) using Eddy’s hot plate method. The AECL produced a significant analgesic activity in a dose dependent manner. All the doses of AECL (250, 500 and 1000mg/kg) had shown analgesic activity. The reaction time obtained for these three doses after 90 minutes of drug administration was found out to be 5.15 mins, 8.92 mins and 10.82 mins respectively which was comparable to Diclofenac sodium (5 mg/kg) that showed the reaction time of 12.36 mins. It was concluded that the AECL has good analgesic potential and may be adopted as alternative to conventional NSAIDS.

Maryam Bincy Thomas   and S.K.Sharma, Lalit Singh   

Cancers of the colon and rectum are the second leading cause of cancer death. Fifty percent of the colorectal cancer occurs in either the lower (sigmoid) colon or the rectum and should be easy to detect at an early stage. The majority of the colon cancers are not inherited, but rather are considered sporadic, having developed from an accumulation of mutations throughout the course of a lifetime. The epidemiological risk factors for cancers, other than genetic risk factors, include dietary components, such as the amount of fat and fiber in the diet, intake of calcium, vitamins of the antioxidant class, NSAIDS such as aspirin and specific inhibitors of cyclo-oxygenase. The risk of colon cancer increases with age, the history of previous polyps or cancer, family history of cancer, history of long standing inflammatory bowel disease including ulcerative colitis and Crohn’s disease. Colonoscopy plays an important role in the medical care of patients with colorectal cancer. It is generally used for both the diagnosis of different stages of colorectal cancer and the treatment of early colorectal cancers and its precursors.

M. Fawzi Mahomoodally   Vidooshi Bhugun   and Geerjanand Chutterdharry   

The incidence of neurodegenerative diseases is rising due to rapidly aging population around the world and it is estimated that by 2040 they would surpass cancer as the principal cause of death in industrialized countries. Neurodegenerative diseases are relentlessly progressive disorders of the central nervous system characterized by cognitive, motor and/or behavioral dysfunctions. These diseases include Alzheimer’s (AD) and Parkinson disease (PD) as most common ones and less commonly amyotrophic lateral sclerosis, Huntington’s disease and vascular dementia. Despite tremendous advances in the understanding of these diseases, pharmacological treatment by conventional medicine has not obtained satisfactory results. For instance, pharmacological therapies for AD such as acetylcholinesterase inhibitors and for PD such as Levodopa are merely symptomatic. This coupled with the fact that they exhibit various side effects have led to the use of complementary and alternative medicine for the management of AD and PD. This review attempts to explore some of the most commonly used complementary and alternative medicine against AD and PD

Laxmikant Zawar and Sanjay Bari 

The aim of the present study was to enhance the solubility, dissolution rate and thus antihyperglycemic activity of a poorly soluble, BCS class II drug repaglinide, using its solid dispersions (SDs) with polyethylene glycol (PEG) 6000. Solid dispersions were prepared by kneading, solvent evaporation, conventional fusion method and microwave induced fusion methods. The dispersions were evaluated for various in vitro parameters such as solubility study, dissolution study, fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray powder diffraction (XRD) and scanning electron microscopy (SEM). Microwave induced solid dispersions exhibited significant improvement in solubility and dissolution rate compared to that of pure drug. Results of DSC, XRD and SEM study showed translation of crystalline form of RG to amorphous form. Thus, microwave technology offers a simple, efficient, solvent free promising alternative method to prepare solid dispersion of RG with significant enhancement of the in vitro dissolution rate.

Emad Y. Moawad 

The goal of this work is to determine the mechanism by which addition of interferon-α (IFN-α ) to Dendritic Cells (DC) grown from Chronic Myeloid Leukemia (CML) patients improves its capacity to stimulate T-lymphocyte responses, and decreases the proportion of bcr-abl positive DC. Bone marrow samples were obtained from six patients with CML and six normal donors to prepare mononuclear cells. T lymphocytes were removed, cultured without IFN-α (control sample) and with IFN-α doses of 5, 50, 250, and 500 U/mL. After a culture period of 14 days, DC were harvested and added to freshly allogeneic T cells by a ratio 1:10 for Mixed Lymphocyte Reaction (MLR) assay to identify energy of those mixed cultures (E_MLR). Fluorescence in situ hybridization (FISH) was performed to quantify the frequency of bcr-abl in fresh samples from newly diagnosed CML patient with cultured DC without IFN-α and with IFN-α dose of 250 U/mL. Variations in E_MLR of mixed cultures were attributed to each of the difference in energy of the cultured DC (EDC) obtained from IFN-αdoses, and either of rising the histologic grade (HG) of those cultures due to cell cycle arrest (ECCA) that cause treatment failure or reducing HG due to energy released by the loss of mitochondrial membrane potential (Ψ_mito ) activating apoptosis in bcr-abl positive cells. Percentage of decrease in bcr-abl positive DC in FISH analysis was 100% identical to that in each of EDC and Ψ_mito (p≤0.001). Patient-specific approaches that account for HG variations should enable more accurate dose estimates. IFN-α therapy is an energy balance process in which CML cells respond according to the mechanism of the following model: E_MLR=H_G + E_DC & ECCA or Ψ_mito = Abs (HG.Control-HG).

Luisa Maria Arvide Cambra 

This paper is a study of fragments of the work entitled in Arabic Tahsil gharad al-qasid fi-tafsil al-marad al-wafid, which was written in the 14th century by the well known Spanish physician Ibn Khatima and which refers to the epidemics of the pest, the terrible pandemic that struck humanity in the 14th century and devastated Asia, Africa and Europe at that time. The article includes an Introduction about the author and the medical and pharmaceutical significance of the work, as well as a section containing the English translation of a few pages of Part VI, according to the Arabic manuscript 1785 from the Library of El Escorial, relating to the treatment of disease, that contain interesting remedies and recipes from the pharmaceutical and the medical points of view.

Karina Sichieri Adriano R.Baldacin Rodrigues Juliana. A.Takahashi Silvia Regina Secoli Moacyr Roberto Cuce Nobre Martinez Altava MĂłnica and Fernández Garrido Julio 

The aims of this systematic review are to identify and analyse the scientist literature available evidence about the use of potentially inappropriate medications, according to the Beers Criteria, that is associated with mortality in the elderly people. It have been made a search of publications in most traditional electronic databases among the scientific community (Pubmed / Medline, EMBASE and Web of Science) and it have been selected publications that obey the criteria of 'observational study', 'elderly' and 'Beers Criteria' and that they had as a result the mortality of the study population. After publications selection it proceeded to dump data by two researchers independently to avoid selection bias. The methodological quality of the selected studies was assessed by the checklist Newcastle-Ottawa. The final sample of this systematic review has been made up of 17 studies published in Pubmed and Embase databases majority, 8 of which make up the meta-analysis. In descriptive synthesis has been observed that most of the studies have a level of evidence IV (94'1%) with cohort delineation (94'1%) and non-probability sampling technique (70'6%).Data collection was prospective in 58'8% of cases, with a sample (n) greater than 1000 elderly (64'7%) and followed up for 6 to 12 months (52'9%).The meta-analysis involving 90.611 elders informed that users who take inappropriate drug according to the Beers Criteria had a higher relative risk for mortality outcome (RR = 1.11, 95% CI 1'01-1'22 P = 0'023), regardless of study stage, comorbidity presence, polypharmacy or type of inappropriate medication used.

Teresa  Pounds Annesha  Lovett Susiana  Eng Khalid  Iqbal Israel  Orija and Jessica  Chmielewski 

In the last two decades, there has been a significant degree of controversy surrounding the use of standardized parenteral solutions. Opponents of standardized parenteral nutrition claim that individualized parenteral nutrition is necessary because the critically ill patient requires daily manipulation of macro- and micro-nutrients secondary to stress associated with complex ailments. The purpose of this study was to determine if premixed parenteral nutrition solutions were equally safe and efficacious, while being less costly, in managing parenteral nutrition of patients at a large metropolitan teaching hospital, as compared to customized parenteral nutrition solutions. This was a randomized controlled trial with no placebo involving 100 patients requiring central parenteral nutrition. Consenting patients received either customized parenteral nutrition or premixed double chamber parenteral nutrition containing protein, carbohydrates and electrolytes. Vitamins and trace elements were added as needed. Each subject enrolled in the study was followed until the parenteral nutrition was either discontinued, the patient was transferred from the facility, or the patient expired during the study. Premixed and customized parenteral nutrition solutions were shown to be equally efficacious in patients as their blood glucose, fluid status, nutritional markers, serum electrolytes, phosphate, and magnesium values were within normal limits (p<.05). Premixed parenteral nutrition is associated with significantly better safety as compared to customized parenteral nutrition [11]. Furthermore, the cost difference was $41,934 when comparing the premixed formulation to the customized solution. In this study, premixed parenteral nutrition solutions were equally safe, effective, and less costly than customized parenteral nutrition formulas. Patients receiving premixed parenteral nutrition experienced less adverse drug reactions and metabolic abnormalities than patients receiving customized parenteral nutrition.

Vivekanand K. Chatap Abhijit M. Karale Pramod Wagh and Prashant K. Deshmukh 

In present investigation attempt was made to designed novel mould with aim to overcome the problems occurs during casting of mouth dissolving films. Placebo and Perindopril Erbumine containing mouth dissolving film (MDF) were prepared with Pullulan, HPMC E-15 as film forming agent and other excipient by solvent casting method on specially design mould and regular petri dish. The HPMC E-15 125mg and Propylene Glycol 30 ÎĽ ml as plasticizer contains MDFs formulation (H2) were found to be optimized when compared with Pullulan on the basis of physical evaluation parameters like weight variation, drug, thickness in the range 0.01-0.03 mm, disintegration time in <17sec. and release of drug from film was found to <60sec and other parameters were found within acceptable limit. The prepared optimized stable mouth dissolving films were characterized by SEM, FT-IR, DSC etc. and various new equipments were used first time in PMDFs preparation for cutting, pill-out and water level indicator for balancing novel mould in oven, which was widely used in other field like engineering and physics. Especially design mould for casting of film was found to be more efficient than regular petri dish due to easy scale up and avoid problems occurs during preparation of stable mouth dissolving film which leads to reduce the wastage of active ingredients and excipients.

John Suttner Annesha White Lovett and Kimberly Vernachio 

The prescribing of opioids for chronic non-cancer pain has escalated over recent years. This pattern has led to a larger number of patients who require discontinuation of opioid therapy. The purpose of this review was to provide an overview of best practices for tapering opioid therapy in patients. A systematic review of the current literature concerning tapering of opioid therapy was performed from 2000-2013. 24 studies were selected for review. Considerable variation was found with regard to taper rate and duration. Taper rate ranged from an initial 20-50% daily reduction in opioid dose to a 5% reduction in dose every one to four weeks. The most common titration rate was a 10% reduction in the daily dose each day. General themes were to individualize taper parameters to ensure patient compliance and presentation of withdrawal symptoms, to slow the rate of the taper to about 1/3 of the original dose, and advise a referral of addicted and complex patients to appropriate specialists for treatment. The majority of available information on tapering opioid therapy consists of clinical guidelines that have been created based on practice experience. There is a need for additional experimental research to develop a more standardized taper protocol.

Lauren Levine Nicole Pallme Erik Angelotti and Dane Shiltz 

The purpose of this retrospective chart review was to determine the correlation between full weight-based enoxaparin use and the frequency of anti-Xa concentrations within the defined therapeutic range; to ascertain if anti-Xa monitoring is being appropriately ordered in relation to the timing of enoxaparin dose (after 3 consistent therapeutic doses and 3-5 hours post-dose); to establish if the evidence-based recommended dose adjustment protocol that was studied in the pediatric population was utilized; and if this yielded anti-Xa concentrations within the target range (0.6 – 1.1 IU/mL) for an adult population. The data may suggest a lack of correlation between BMI and whether or not the anti-Xa concentration is within the therapeutic range. Further prospective studies are needed to confirm this finding, and to determine the utility of the available dose adjustment nomogram.

Pilar PĂ©rez-Ros Francisco MartĂ­nez-Arnau Esther Navarro-Illana Inmaculada Tormos-Miñana and Francisco JosĂ© Tarazona-Santabalbina 

Introduction: The risk of falling increases with age. A third of the population over 65 has one or more falls per year. Objective: to know the relationship between drug prescription and falls in the elderly. Materials and Methods: a study was carried out through a community intervention in individuals ≥ 70 years of age. Results: the sample was composed of 249 participants, 160 women (64%), with a mean age of 74.47 years (SD 5.33). During the 12 months prior to the study, the mean of falls per person was 0.5 (SD 0.94), the mean of the risk factors was 2.73 (SD 1.4) and the mean of the medication prescribed was 4.2 (SD 3.0). The percentage of the reduction of falls after the study was 12%. The amount of medication prescribed correlated with the incidence of falls before and after the study, r=0.193, p=0.002 y r2=0.170, p=0.009, respectively. Prior to the study, the individuals who were prescribed beta-blockers and antidepressants, had a fall incidence of 0.74 (SD 1.14) and 1.22 (SD 1.09), respectively, however after the intervention there was no relationship between drug prescription and falls. Conclusions: the fall prevention community program was effective since it prevented the negative effects of medication on falls. An interdisciplinary community intervention reduces the global incidence of falls and the incidence of falls related to some specific medication.

Dibyajyoti Saha 

Outsourcing pharma or biotech research information technology (IT) can be very difficult to implement but with a well-planned strategy the benefits can easily outweigh the risks. Discovery R&D operations can often be chaotic because of intense financial pressures, immature processes and lack of engineering support. Effective IT implementation needs to adapt to this reality and cater to scientific rather than technological goals. An effective discovery IT strategy does not operate in a vacuum and is guided by periodic productivity measures. This feedback loop is the gatekeeper for taking on new ground.

Vivekanand K. Chatap Abhishek R. Maurya Prashant K. Deshmukh and Laxmikant R Zawar 

Nisoldipine (NSD) is a calcium channel blocker used for treatment of angina pectoris, hypertension and congestive heart failure etc. It belongs to BCS class-II i.e., low solubility & low bioavailability (3.7 to 8.4%) due to extensive pre-systemic metabolism of NSD. Therefore, this research work was carried out with aim to improve solubility and bioavailability. NSD sublingual tablets were prepared by direct compression method with two biodegradable polymer as major components, pullulan as solubility enhancer & chitosan used to reduce flushing action of saliva and further evaluated pre & post-compression parameters, in-vitro drug release study and characterised by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) & Fourier transform infrared spectroscopy (FTIR). It was observed that, formulation F3 containing 3 % w/w of pullulan and 4% w/w chitosan showed satisfactory results with disintegration time of 34 second, wetting time of 20 second and dissolution (98.45%) in 45 min. The DSC, XRD & FTIR studies showed no interaction between drug and polymer or with other additives. For rapid absorption and high bioavailability, with subsequent almost immediate onset of pharmacological effect. From this study, It can be concluded that, drug having low solubility and low bioavailability due to pre-systemic metabolism can be improve by cost effective, easy to scale up sublingual oro-mucosal approach.

S.M. Zahid Hosen Swati Paul and Dibyajyoti Saha 

In 21th century, the human being has gained the ability to make the clone of natural things and one of the most wonderful examples is fake egg production which is looked real as the original one. Fake egg or artificial egg is made by using various types of raw materials, colors and flavors. Normally eggs provide about six grams of protein-half of this protein is in the egg white. Most of the nutrients in eggs are found in yolk. But artificial eggs are full of chemicals, additives and auxiliary agents. So fake eggs contain no nutritional values compared to the real eggs. In China it was claimed in various news that fake eggs are sold in the local market because of money. The chemicals used for artificial eggs causes metabolic disorders, brain damage, liver disease, cancer and many other diseases . So the productions of fake eggs haven’t any health benefit rather it’s a chemical hazard. Generally the artificial creation of natural things doesn’t blessing for human being.

Maryam Bincy Thomas Kashif Khan S. K. Sharma Lalit Singh and M K Upadhyay 

The present study was carried out to evaluate the in vitro antimicrobial and antioxidant activity of Emblica officinalis juice powder. The antimicrobial activity was assessed against gram positive and gram negative bacteria namely E.coli, Pseudomonas fluoresces, Bacillus subtilis, S.aureus, and fungi namely Aspergillus niger, Penicillium chrysogenum, Alternaria alternata, and Fusarium spp by agar well diffusion method. The antioxidant activity of the powder was determined in vitro using hydrogen peroxide scavenging activity method. The amount of total phenolic content was also determined by Folin Ciocalteau method. The result of the study revealed antibacterial and antioxidant activity. The Emblica officinalis powder showed no antifungal activity against the tested strains. The activity was found to be concentration dependent. The results of present study conclude that Emblica officinalis juice powder possess high antibacterial and antioxidant activity and can be further explored for the isolation of its bioactive compound.

Nuala Helsby Michael Goldthorpe Peter Gow and Janak de Zoysa 

Cyclophosphamide treatment of lupus nephritis is associated with ovarian toxicity. Four separate studies have previously demonstrated a lower risk of cyclophosphamide induced premature ovarian failure (POF) in carriers of the CYP2C19*2 null function allele. This hepatic enzyme bioactivates cyclophosphamide. CYP2B6 is also important in the activation of this prodrug however, genetic variants of CYP2B6 have not been associated with POF risk. The aim of this study was to determine the relationship between CYP2C19 and CYP2B6 loss of function variants and prevalence of ovarian toxicity following treatment with monthly pulses of intravenous cyclophosphamide in lupus nephritis patients. In 28 pre-menopausal female patients, there was a 25% incidence of POF. In contrast to previous studies of a similar size we could not detect a significant relationship between the risk of POF and genetic variants of CYP2C19, alone or in combination with variants of CYP2B6. However, 71.4% of the cases with POF had been treated with additional daily oral cyclophosphamide compared with only 4.7% of controls (P < 0.02; OR 14.29 (95% CI, 1.4-144.5). Thus the effect of daily oral cyclophosphamide administration in addition to pulsed intravenous monthly doses may have obscured any protective effect of CYP2C19 loss of function in this cohort.