Alginate/chitosan nanoparticles for improved oral delivery of rifampicin: Optimization, characterization and in vitro evaluation

Abstract

Alginate/chitosan nanoparticles were synthesized by ionotropic method using natural honey as the stabilizing agent. The nanoparticles were characterized and the potential of these nanoparticles for the controlled oral delivery of antitubercular drug rifampicin was evaluated in terms of entrapment efficiency, swelling behaviour and in vitro release of the drug. Carboxyl content and in vitro cytotoxicity of the nanoparticles were also evaluated. The swelling and in vitro drug release indicates that the system undergoes pH-dependent swelling and release of drug. Drug release was very low in acidic pH and a maximum of only 20 % of the drug was released in 5 h. A sustained release of drug was observed at pH 7.4 and complete release was obtained in 8 h. Kinetics of the drug release was analyzed by fitting the experimental data into Korsmeyer-Peppas equation and show that the mechanism involved in the release was non-Fickian, controlled by a combined mechanism of diffusion and polymer relaxation. This study shows that the obtained nanoparticles can be a potential carrier for the pH controlled oral delivery of rifampicin.