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 |
Parkinson’s disease is the second most common progressive, age-linked neurodegenerative disorder. The sporadic form of the disease is usually idiopathic, where mitochondrial dysfunction is its major hallmark. Mitochondria are multifunctional dynamic organelles that carry out major cellular functions that get damaged by reactive oxygen species, deposition of lewy bodies, dopaminergic neuronal cell death, mitochondrial DNA mutations, and imbalance in fission/fusion that ultimately weakens mitophagy. In this review, the updated key roles and mechanisms of mitochondrial dysfunction structurally and functionally in the pathogenesis of sporadic Parkinson’s disease are discussed to understand the process of neurodegeneration. Research Data from numerous studies confirm mitochondrial dysfunction being the Basis of the disease. Here, we briefly bring the overview of illicit drug administration, oxidative stress, mitochondrial DNA mutations, mitochondrial genome mutations, alpha-synuclein aggregation, mitochondrial dynamics-fission and fusion, and the impairment of mitophagy in the disease pathogenesis. In conclusion, understanding mitochondrial dysfunction and its pathways can be a major target in treatment and prevention of Parkinson’s...
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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 |
The concept of Quality by Design reflects current global regulatory thinking related to pharmaceutical products. The pharmaceutical industry needs to improve its performance. Newer technologies need to be implemented that can effectively reduce the cost and, at the same time, improves product quality. Quality by design (QbD) is the best solution to build quality in all pharmaceutical products. The main objective of QbD is to ensure the quality product resulting from a combination of prior knowledge and new estimation during development. QbD is being widely promoted by the food and drug administration (FDA) and the international conference on Harmony (ICH). Quality by design (QbD) in the pharmacy field is mainly based on the understanding of how materials and process parameters affect the quality profile of final products. In this article, the key elements of QbD viz., Target product quality profile, Critical quality attributes, Risk assessment, Design space, and Control strategy are discussed to understand the performance of dosage forms within the design space. Tools of QbD (DoE, Quality risk...
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