Optimization and Characterization of Artesunate-Loaded Chitosan-Decorated Poly(D,L-lactide-co-glycolide) Acid Nanoparticles

Abstract

The aim of this study was to optimize the formulation of artesunate-loaded chitosan-(CS-) decorated poly(D,L-lactide-co-glycolide) acid (PLGA) nanoparticles as well as evaluate their characteristics. CS-to-PLGA mass ratio, pH of CS solution, and experimental temperature were optimized using response surface methodology to understand their effects on size and zeta potential of nanoparticles. The optimized formulation showed the close agreement between predicted and experimental values (all bias below 5%). The presence of CS was confirmed by positive surface charge and Fourier transform infrared spectroscopy. A spherical-like shape of particles was observed in range of small size around 190 nm. This CS layer restricted initial burst release of drug from carriers in phosphate buffer of pH 6.8. In addition, CS-coated NPs enhanced the intracellular uptake, in vitro cytotoxicity, and apoptosis-induced nuclei behaviors compared with CS-uncoated NPs as well as free drug in MCF-7 and A549 cancer cells.