Abstract
The present study was planned to apply the nanotechnology to therapeutically proven flavonoid-rich fraction for obtaining a formulation with enhanced antihyperglycemic activity. The leaves were extracted in aqueous-methanol and fractionated to yield a flavonoid-rich fraction. This fraction was formulated into an aqueous nanosuspension using PVA through the nanoprecipitation method. The developed formulations were characterized for physical parameters and optimum nanosuspension was evaluated against type 2 diabetes in high-fat diet-fed, streptozotocin-induced diabetic animals. The pharmacokinetic parameter and histopathology were assessed to determine the kinetic profile and tissue architectures post oral administration of selected nanosuspension. The selected nanosuspension was also studied for stability under accelerated conditions. Flavonoid-rich fraction was obtained using Kupchan partitioning. The developed nanosuspension PG-EA–NS–B showed optimum physical parameters. In hyperglycemia induced by streptozotocin, in high-fat diet-fed rats, it effectively restores the normal level of blood glucose in the first hour. The effects were comparable to standard Glibenclamide. In biochemical observations, PG-EA–NS–B, as well as PG-EA, showed beneficial effects on various hepatic and renal parameters. The pharmacokinetic parameters showed that nanosuspension enhances the absorption and decreases the metabolism of flavonoid actives. The selected nanosuspension and free flavonoid fraction showed rectification of histological changes. The nanosuspension was most stable in cool conditions. PVA based nanosuspensions can be a viable strategy for oral delivery of natural flavonoids, as it significantly affected the absorption and metabolism of flavonoids upon oral administration.
Published Version
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