In this study, we prepared chitosan-coated Poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles. Specifically, we utilized a double emulsion-solvent evaporation technique to formulate nanoparticles containing paclitaxel as a model macromolecule and 6-coumarin as a fluorescent marker. SEM images verified that all nanoparticles were spherical in shape with smooth surfaces. Chitosan coating slightly increased the size distribution of the PLGA/PVA nanoparticles, from 202.2+/-3.2 nm to 212.2+/-2.9 nm, but the encapsulation efficiency was not significantly different. In contrast, coating with chitosan slowed the in vitro drug release rate and significantly changed the zeta potential from negative (-30.1+/-0.6 mV) to positive (26+/-1.2 mV). At the initial burst time, the drug release rate from chitosancoated nanoparticles was slightly slower than that of the uncoated nanoparticles. Chitosan-coated nanoparticles were also taken up much more efficiently than uncoated nanoparticles. This study demonstrated the efficacy of chitosancoated PLGA nanoparticles as an efficient delivery system.