OBJECTIVE To formulate atractylodin-loaded poly (lactic- co- glycolic acid) (PLGA) nanoparticles and characterize the prepared nanoparticle formulation.METHODS The nanoparticle formu-lation was developed using solvent displacement method. The encapsulation and loading efficiency were characterized and particle size, and zeta potential were determined by dynamic light scattering technique.Drug release was assessed in vitro.RESULTS The size(mean±SD of diameter)of the prepared atractylodin-loaded PLGA nanoparticles were (161.27 ± 1.87)nm with narrow size distribution (mean PDI: 0.068±0.015)and zeta potential(28.83±0.35)mV.The encapsulation and loading efficiency were (48.31±0.83)% and(2.15±0.04)%,respectively.Drug release from atractylodin-loaded PLGA nanoparticles was observed up to (87.70 ± 0.47)% in 72 h with biphasic manner. Moreover, the nanoparticles were found to be freely dispersible in water without aggregation. CONCLUSION Results suggest that PLGA nanoparticles may be used as an effective drug delivery system for atractylodin.The anti-cholangiocar-cinoma activity of this nanoparticle formulation is required.