This article describes the preparation and characterization of anticancer drug-loaded poly(lactide-co-glycolide) (PLGA) microparticles. PLGA microparticles loaded with doxorubicin HCl (DOX) were prepared via o/w emulsion solvent evaporation. The release characteristics, encapsulation efficiency, size, and morphology of the PLGA microparticles were also determined. A cytotoxicity test was performed by using Glioma RG2 cancer cells to investigate the cytotoxicity of DOX-loaded PLGA microparticles. The DOX-loaded PLGA microparticles had an average diameter of 500 +/- 9 nm. The DOX encapsulation efficiency and drug loading were 22.75% and 0.78%, respectively. DOX-loaded PLGA microparticles displayed a significant cytotoxicity toward the RG2 cells as compared to the unloaded PLGA microparticles.