Abstract

DESIGN, FORMULATION, AND OPTIMIZATION OF YOHIMBINE HYDROCHLORIDE PLGA NANOPARTICLES BY EXPERIMENTAL DESIGN APPROACH

*Dr. A. Sambasivarao M.S Ph.D, G. Lakshman, Mathe Ark, V. Bhumika

ABSTRACT

Yohimbine has demonstrated significant therapeutic potential, serving as an anti-inflammatory, anticancer, and fat-burning agent. Nonetheless, yohimbine's clinical usefulness is hampered by a number of pharmacokinetic constraints, including limited solubility, insufficient bioavailability, and high hepatic first-pass metabolism, which all reduce its therapeutic effects. However, oral yohimbine's therapeutic efficacy Its application is limited because to weak solubility, low bioavailability, and hepatic first. The goal of this work is to create yohimbine-loaded PLGA nanoparticles (YBN-PLGA) that improve yohimbine release, oral bioavailability, and anti-fibrotic activity. We created YBN-loaded PLGA nanoparticles using a combined emulsification and solvent evaporation process. The formulation was optimized by conducting a comprehensive evaluation of both formulation and processing factors. The improved formulation was studied using Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and powder X-ray Diffraction (p-XRD). The improved formulation of YBN-loaded PLGA nanoparticles had a particle size of 210 nm, a PDI of 0.01, a zeta potential of -34 mV, and 64% entrapment efficiency. Notably, our experiments show that this formulation has a longer-lasting YBN release profile than pure yohimbine hydrochloride under simulated gastrointestinal and physiological buffer conditions, which we attribute to the inclusion of PLGA. The YBN-loaded PLGA nanoparticles showed an appropriate particle size for oral administration, which may improve bioavailability and potentially increase therapeutic efficacy in the treatment of fibrotic diseases. 

Keywords: polymeric nanoparticles, Yohimbine, sustained release, PLGA.