Optimisation and evaluation of Gymnema sylvestre extract loaded polymeric nanoparticles for enhancement of in vivo efficacy and reduction of toxicity

Aim This work studies the development and evaluation of Gymnema sylvestre (GYM) extract loaded sustained release polymeric nanoparticles (PNPs) for enhanced bioavailability and reduced nephrotoxicity. The current therapy is associated with the drawbacks of addiction and repeated administration. Method The sustained release PNPs were developed and evaluated for toxicity. PNPs of GYM were prepared by double emulsion solvent evaporation technique utilising Taguchi model and evaluated for physicochemical properties (particle size, zeta potential, entrapment efficiency), in vitro drug release, compatibility, and stability. Further, the bioavailability and in vivo nephrotoxicity studies in diabetic rat model were also carried out. Result The developed optimised nanoparticles were 205.7 +/- 1.20 nm in size, -40.68 mV zeta potential, compatible, and stable in nature with improved entrapment efficiency (67.1 +/- 0.2%) and sustained release. Moreover, nanoparticles were found to lower the blood glucose level in single as well as multiple doses. Results of in vivo study indicated that GYM-NPs increased the phosphorylase activity and thus enhanced insulin secretion. Furthermore, the nanoparticles were free from toxicity, which was confirmed by the estimation of kidney biomarker. Conclusion The nanoparticles increased the bioavailability of GYM extract and have a great potential for the treatment of diabetes in reduced dose, and so these can be potential candidates for treating diabetes.