FORMULATION AND IN VITRO EVALUATION OF NANOPARTICULATE MATRIX TABLET OF NEBIVOLOL HYDROCLORIDE

Abstract

RETRACTED

Beta blockers are widely used in treatment of hypertension. Nebivolol have greater selectivity for β1-adrenergic receptors and have ability to stimulate endothelial nitric oxide production, leading to vasodilation. But, it undergoes extensive first pass hepatic metabolism and varying half-life along with low aqueous solubility. The objective of present study is to develop nanoparticulate matrix tablet containing Nebivolol hydrochloride. Nebivolol nanoparticles are prepared by solvent evaporation method using varying concentration of drug and polymer Eudragit RL 100. The physicochemical study confirmed the particle size in nano range with smooth morphology and FTIR spectroscopy, DSC studies confirm compatibility of drug and polymer. Nanoparticulate matrix tablet was prepared by direct compression method using varying concentration of nanoparticles and ethyl cellulose. The matrix tablets were found within specification limits for various physicochemical parameters. The in vitro drug release in 0.1N HCl and phosphate buffer pH 6.8 showed prolongation of drug release. The mechanism of drug release from nanoparticulate matrix tablets followed diffusion process based on fickian diffusion and super case II transport. Stability studies showed no changes after exposing to accelerated conditions for a period of 3 months as per ICH guidelines. The grouping of nanoparticles in matrix system had an enormous impact on drug release rates, which can diminish the plasma drug variance, extensive first pass effect and variable elimination half-life.