Formulation and Evaluation of Polymeric Nanoparticles as Carriers of Rosuvastatin Calcium for Oral Administration

Abstract

Aim of this research was to formulate and evaluate the polymeric nanoparticle as carriers of rosuvastatin calcium for oral administration. Rosuvastatin calcium-loaded nanoparticles were formulated by nanoprecipitation method using different ratios of polymers (Eudragit L100 and Eudragit S100) and different concentrations of stabilizers (Pluronic F68 and PVA) with constant drug concentration. The formulations were evaluated for particle size, zeta potential, drug content, entrapment efficiency, in vitro release, kinetics, solubility, ex vivo intestinal permeability and Transmission Electron Microscopy (TEM). Fourier Transform-Infrared (FT-IR) spectroscopy and Differential Scanning Calorimetry (DSC) studies were carried out to check compatibility between the drug and polymers. No significant drug-polymer interactions were found. To enhance drug entrapment particle size range from 100-250 nm were prepared and entrapment efficiencies were found be 28-79 %. In vitro release studies showed a biphasic release pattern of rosuvastatin calcium from nanosuspensions: One initial burst release in the first 2 hours which could be helpful to improve the penetration of drug followed by a second slow release phase consistent with a Higuchi diffusion mechanism. The solubility of rosuvastatin calcium loaded polymeric nanoparticles compared to pure drug form was increased to about two-fold. Intestinal permeability of rosuvastatin calcium entrapped in Eudragit L100 an Eudragit S100 nanoparticles across rat small intestinal segments was significantly improved compared with rosuvastatin calcium in solution. Nanoparticles observed by TEM showed extremely spherical shapes. Results indicated that nanoparticle formulations could be a promising delivery system for oral administration of rosuvastatin calcium with enhanced solubility, intestinal permeability and improved oral bioavailability.