Abstract: Objective:To prepare curcumol PEGylated liposomes and to investigate the characterization of curcumol PEGylated liposomes in vitro. Methods:Curcumol PEGylated liposomes were prepared with thin-film dispersion technology. The morphology, particle size, zeta potential, stability and release profile of curcumol PEGylated liposomes in vitro were observed. The cellular uptake and cytotoxicity were determined in vitro. Results:Three batches of PEGylated liposomes of curcumol were prepared. Most of them were round ball and the average particle size was (150.3±4.0) nm, the PDI value was 0.197±0.009, and the zeta potential was (-24.5±0.7) mV. The average entrapment efficiency of the curcumol PEGylated liposomes was 80.24%.There was no significant change in the drug content and the particle size after 2 months of storage at 4℃. In the cellular uptake experiment, PEGylated liposome loaded coumarin-6 could enhance the uptake of MDA-MB231 cells. The PEGylated liposomes of curcumol had strong cytotoxic effect on MDA-MB231 cells, and its effect was stronger than that of curcumol liposomes and free curcumol. Conclusion:Curcumol PEGylated liposomes were obtained with high entrapment efficiency and good stability. Curcumol PEGylated liposomes could enhance the uptake and cytotoxicity of breast cancer MDA-MB231 cells in vitro.