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Withania somnifera Dunal is an Indian medicinal plant with significant pharmacological properties, such as adaptogenic, anti-inflammatory, anti-oxidant, anti-platelet, anti-hypertensive, hypoglycemic and hypolipidemic effects. Several chemotypes of W. somnifera include NMITLI-101, NMITLI-118 and NMITLI-128. The present work elaborates the optimization and development of a liposomal delivery system for efficient delivery of NMITLI118RT+ [a standardized ethanolic extract of a new chemotype of W. somnifera Dunal (NMITLI-118) roots] against cerebral stroke in rats. Liposomal systems were prepared using thin-film hydration method and characterized on the basis of size, zeta potential, physical stability, FT-IR, DSC-TGA analysis and surface morphological studies by TEM. NMITLI118RT+ and its formulations (NMITLI118RT+LF) were evaluated for biological activity utilizing middle cerebral artery occlusion model in rats. The Z average of the developed liposomal formulation was about 142.6 ± 0.09 nm with a zeta potential of −31.20 ± 1.0 mV. Results of TEM revealed spherical particles in the range of 200 nm. The entrapment efficiency was found to be 94.603 ± 2%. The formulation was found to be physically stable over a 3-week period. Results were suggestive of the fact that both NMITLI118RT+ and its delivery system possess significant neuroprotective activity in cerebral ischemia. The liposomal system largely exhibits better performance over NMITLI118RT+ precisely in the post-treatment group. The present studies could elucidate the successful development of a delivery system for NMITLI118RT+ and demonstrate their beneficial neuro-protective potential in overcoming and reversing the consequences of I/R injury following stroke.

Diabetes mellitus had emerged as a metabolic menace which leads to the development of dyslipidemia, myocardial infarction, coronary artery diseases, obesity and hypertension. These are critical hallmarks for severe metabolic disorders owing to lack of proper balance between the energy intake and energy consumed. Previously, various potent biomarkers were investigated for their remarked potential against diabetes as well as hyperlipidemia. With this contextual, we synthesized different phytomolecular hybrids from the known potent biomarkers lupeol, β-sitosterol, ursolic acid, gallic acid and cinnamic acid by esterification with dicyclohexyl-carbodiimide as a coupling reagent and 4-dimethylaminopyridine as a catalyst. The compounds were purified using column chromatography and identified by mass spectroscopy, IR spectroscopy, NMR spectroscopy (1H and 13C).Through in vitro screening by α-amylase assay and antioxidant assay, PMH1, PMH2 and PMH4 were found as effective phytomolecular hybrid compounds that displayed potential anti-diabetic, anti-hyperlipidemic as well as anti-oxidant properties. Amongst them, PMH4 prevailed in inhibiting the adipocyte differentiation. Our findings showed significant antidiabetic (STZ model in rats), antihyperlipidemic and antioxidant outcomes by PMH4. Synthesized phytomolecular hybrids with known potent biomarkers can be an effective strategy to design new interventions with effective bioactivity to elicit prominent in vivo performance.HighlightsPhytomolecular hybrids from the known potent biomarkers lupeol, β-sitosterol, ursolic acid, gallic acid and cinnamic acid were synthesized by esterification with dicyclohexylcarbodiimide as a coupling reagent and 4-dimethylaminopyridine as a catalyst.Synthesized effective phytomolecular hybrid compounds were screened for potential anti-diabetic, anti-hyperlipidemic as well as anti-oxidant properties invitro assays.Synthesized effective phytomolecular hybrid PMH4 prevailed in inhibiting the adipocyte differentiation and displayed significant antidiabetic (STZ model in rats), antihyperlipidemic and antioxidant outcomes.Synthesized phytomolecular hybrids with known potent biomarkers can be an effective approach to design new interventions with effective bioactivity Phytomolecular hybrids from the known potent biomarkers lupeol, β-sitosterol, ursolic acid, gallic acid and cinnamic acid were synthesized by esterification with dicyclohexylcarbodiimide as a coupling reagent and 4-dimethylaminopyridine as a catalyst. Synthesized effective phytomolecular hybrid compounds were screened for potential anti-diabetic, anti-hyperlipidemic as well as anti-oxidant properties invitro assays. Synthesized effective phytomolecular hybrid PMH4 prevailed in inhibiting the adipocyte differentiation and displayed significant antidiabetic (STZ model in rats), antihyperlipidemic and antioxidant outcomes. Synthesized phytomolecular hybrids with known potent biomarkers can be an effective approach to design new interventions with effective bioactivity

Background: Flavonoid-rich extract of the plant is long known for its anti-diabetic activities in traditional medicine. S002-853, a new flavone derivative synthesized by Central Drug Research Institute (CDRI) has been used for the present study. Objectives: The present study aimed at development of an assay method for quality control (QC) and stability studies of a new anti-diabetic and anti-dyslipidemic agent CDRI compound S002-853. Materials and Methods: A validated high-performance liquid chromatography analysis method for S002-853 was developed for in process QC and stability studies. The separation was achieved on a RP-C18 (25 cm × 0.4 cm, 5 μm, Phenomenex) at 240 nm with flow rate of 1.0 ml/min. This method was applied successfully in establishing forced degradation and drug-excipient testing protocols as per International Conference on Harmonization guidelines. Results: The result of estimation and stress testing studies indicated a high degree of selectivity of this method. S002-853 was most stable at pH 7 and under photolytic conditions. The temperature degradation pattern of S002-853 was found to follow the zero order degradation. Conclusion: The method described is easy and simple hence can be easily reproduced. This method can be very useful for bulk manufacture QC, and drug development process.