Chitosan-sodium Alginate Nanoparticle as a Promising Approach for Oral Delivery of Rosuvastatin Calcium: Formulation, Optimization and In vitro Characterization

Abstract

Rosuvastatin calcium is the most effective antilipidemic drug and is called "super-statin" but it exhibits low aqueous solubility and poor oral bioavailability of about 20%. The present work aimed to develop and optimize chitosan-alginate nanoparticulate formulation of rosuvastatin which can improve its solubility, dissolution and therapeutic efficacy. Chitosan-alginate nanoparticles were prepared by ionotropic pre-gelation of an alginate core followed by chitosan polyelectrolyte complexation and optimization was done in terms of two biopolymers, crosslinker concentrations. The chitosan-alginate nanoparticles were characterized by various techniques such as particle properties such as size; size distribution (polydispersity index); Zeta-potential measurements and Fourier transform infrared spectra respectively. The designed rosuvastatin loaded chitosan-alginate nanoparticle had the average particle size of 349.3 nm with the zeta potential of +29.1 mV, and had high drug loading and entrapment efficiencies. Fourier transform infrared spectra showed no chemical interaction between the rosuvastatin and chitosan-alginate nanoparticle upon the encapsulation of rosuvastatin within the nanoparticles. Nanoparticles revealed a fast release during the first two hours followed by a more gradual drug release during a 24 h period. Hence, our studies demonstrated that the new chitosan-alginate nanoparticle system of rosuvastatin is a promising strategy for improving solubility and in turn, the therapeutic efficacy of rosuvastatin. Therefore, the rosuvastatin-loaded chitosan-alginate nanoparticles are a promising approach for the oral delivery of rosuvastatin.