Formulation And Evaluation Of Metformin-Loaded Nanoparticles For Enhanced Oral Bioavailability And Antidiabetic Activity

Abstract

The present study aimed to create and evaluate nanoparticles encapsulating metformin to enhance its antidiabetic efficacy and oral bioavailability. The PLGA polymer was employed in the solvent evaporation method to produce nanoparticles. We assessed the in vitro drug release, zeta potential, drug entrapment efficiency, and particle size of the synthesized MTF-NPs. The improved formulation exhibited an entrapment effectiveness of 84.7 ± 2.1%, a mean particle size of 178.3 ± 4.2 nm, and a zeta potential of −22.6 ± 1.3 mV. The medication exhibited a release of 82.5 ± 3.5% of its total volume over 24 hours in in vitro release assays, demonstrating a biphasic release profile characterized by an early burst followed by sustained release. The oral bioavailability of MTF-NPs was demonstrated to be 2.6 times greater than that of standard metformin, based on pharmacokinetic testing in rats. Following 14 days of treatment, MTF-NPs significantly reduced blood glucose levels by 62.8% in streptozotocin-induced diabetic rats, in contrast to a 35.4% reduction observed in the metformin group, thereby exhibiting in vivo antidiabetic efficacy. Histopathological study of pancreatic tissues indicated that islet architecture was enhanced in the group treated with nanoparticles. This research offers additional evidence that employing metformin-loaded nanoparticles to enhance the therapeutic efficacy and oral bioavailability of diabetes medicines is a feasible approach.