Posted by admin on May 31, 2022 in |
Febuxostat (FXT), used for treating gout, is poorly soluble and is susceptible to enzymatic degradation when administered as tablets. The current study aims to formulate, optimize and develop a stable Liquid self-nanoemulsifying drug delivery system (L-SNEDDS) and Solid SNEDDS to improve solubility, resulting in enhanced bioavailability and further to formulate Self-Nano emulsifying Osmotic Pump Tablets (SNEOPT) for controlled drug release. A ternary plot was constructed with Capmul MCM (oil phase), Tween 80 (surfactant), and PEG 400 (co-surfactant). Further optimization was done by D-Optimal design. Optimized L-SNEDDS (F8) was then converted to S-SNEDDS by the adsorption method. Aerosil 200 was used as an adsorbent. The L-SNEDDS and S-SNEDDS were characterized and evaluated. The particle size of the optimized batch was 97.25 nm (L-SNEDDS) and 155.2 nm (S-SNEDDS). In-vitro dissolution studies showed>75% release in pH 1.2 HCl buffer and >80% in phosphate buffer pH 7.4 in 1 hour. SEM (Scanning electron microscopy) studies indicated spherical particle morphology. SNEOPT was prepared by direct compression (with NaCl as the osmogent). In-vitro release from...
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Posted by admin on May 31, 2022 in |
Computational chemistry is a robust and economical tool for designing and developing potent therapeutic molecules. Benzimidazole and its analogues are compounds with a unique pharmacophore that derives its application as broad-spectrum antimicrobial agents. A quantitative structure-activity relationship (QSAR) study was performed using a data set of 28 benzimidazole analogues with antimicrobial activity. Descriptors were generated using various free software’s such as PaDEL-Descriptor, SwissADME and OCHEM (Online chemical modelling environment). The statistical analysis was performed using the Stats. Blue software by multiple linear regression (MLR) method for determining the relationship between dependant variable and various independent variables. The best QSAR model had an r2 value of 0.6773, and the predictive r2 value for external validation was 0.7150. The results show that a positive correlation is established between the descriptors, TPSA (Topological polar surface area), H-bond acceptors, iLOGP (Implicit LOGP), GGI4 (Galvez topological charge indices of order 4), thereby achieving the most accurate...
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Posted by admin on May 31, 2022 in |
Phyllanthus niruri commonly known as Keezhanelli is traditionally used as a medicinal plant in many parts of the world. In this study, phytochemical screening was the hepatoprotective potential of the plant investigated. Two plant forms, namely, dry powder and fresh leaves were used. Aqueous and methanolic extracts were prepared from both forms, and the experiments were carried out. The hepatoprotective potential of the Phyllanthus niruri extracts was evaluated by checking the enzyme activity in CCl4 toxicity-induced chicken liver. The liver was subjected to different extracts and the SGPT, LDH levels were calculated. The methanolic extracts displayed higher SGPT levels in the liver after CCl4 treatment (~121 IU/L) while the dry powder aqueous extracts were the lowest (79.5 IU/L). The LDH levels were the highest for fresh leaves methanolic extracts (323.23 IU/L) while the dry powder aqueous extracts (303.01 IU/L) had the lowest level among all extracts. Thus the fresh leaves methanolic extract was proven to be the most efficient out of all of the Phyllanthus niruri extracts. All of...
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Posted by admin on May 31, 2022 in |
During the past few years, diabetes has been one of the leading metabolic disorders. It occurs when the body does not produce enough insulin or the body cells are not efficient enough to take up the insulin. This increases blood glucose levels that affect the body system, particularly blood vessels and nerves. Due to the side effects of allopathic medicines, individuals are searching the other alternatives with lesser side effects and more efficacy. Such properties are present in plant-based product. Picrorhiza kurroa Royle ex. Benth. belonging to the family Plantaginaceae/Scrophulariaceae distributed in Himalayan regions of China, Pakistan, India, Bhutan and Nepal. The tribes of North–Eastern Himalayan regions of India use this herb as for controlling diabetes. The present study was conducted to evaluate the antidiabetic activity of ethanolic extract of P. kurroa in-vitro and in-vivo. In-vitro antidiabetic activity was done by inhibiting the alpha-amylase enzyme, which is hydrolyzing enzyme for the starch by plant extract. In-vivo antidiabetic activity was done by injecting alloxan monohydrate (120 mg/kg bw) to male...
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Posted by admin on May 31, 2022 in |
Obesity and overweight have recently drawn greater attention due to their central role in the rapid increase of metabolic syndrome disorders. The research pursuit for exploring novel and effective therapeutic alternatives to deal with obesity ailments and oxidative stress has received immense interest. In this study, different solvent fractions of Nigella sativa (N. sativa; Black cumin) seeds were prepared and their phytochemical analysis was done. Among different solvent fractions, the methanolic fraction of N. sativa (MFNS) contained a high level of polyphenols (451.77 ± 0.91 μg/mL) and flavonoids (401.24 ± 0.73 μg/mL). The GC-MS analysis of MFNS showed the presence of several glycosides, oils, and polyphenolic compounds, as mentioned in the results section. The effect of N. sativa seed fractions on inhibition of key digestive enzymes linked to adiposity such as α-amylase, α-glucosidase and pancreatic lipase was evaluated. The free radical scavenging activity of seed fractions was studied through standard antioxidant assays (DPPH and NO). The enzyme inhibitory effect of MFNS for α-amylase, α-glucosidase and pancreatic lipase was 81.47%,...
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