Rifampicin Loaded Chitosan-Based Nanoparticles: Optimization, Characterization, and Mucoadhesion

Abstract

One of the important problems in modern pharmaceutical technology is the development of effective and safe drug delivery systems. In this regard, the development of nanostructures that deliver drugs in a targeted manner and increase their bioavailability is of particular importance. Biodegradable polymers form the basis of such systems. Among natural polysaccharides, chitosan deserves special attention. Colloidal particles made from chitosan, especially nanoparticle-based systems, increase the solubility of drugs and enable their effective delivery through the mucosal layer. This study aimed to prepare chitosan nanoparticles loaded with an anti-tuberculosis drug (rifampicin) using the ionotropic gelation method. A central composite design (CCD) was used to study the effects of chitosan concentration, rifampicin concentration, medium pH, and ethanol volume on particle size, polydispersity, and nanoparticle yield. The optimized nanoparticles were spherical in shape with an average particle size of 386±9 nm and a polydispersity index of 0.259±0.025. The rifampicin loading and nanoparticle yield of the optimized nanoparticles were 20 % and 71 %, respectively. The produced nanoparticles were analyzed using thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC), and the results showed no interaction between the drug and the polymer. Drug release from the polymer matrix was studied at different pH values stimulating the gastrointestinal tract. The mucoadhesive activity of rifampicin-loaded chitosan nanoparticles was investigated through the interaction with mucin in acetate buffer solution (pH 5.5) and phosphate buffer solution (pH 6.8). The results showed higher mucoadhesive activity in an acetate buffer solution.