莪术醇长循环脂质体的制备及体外抗乳腺癌作用研究

目的:制备莪术醇长循环脂质体并对其体外性质进行初步研究。方法:用薄膜分散法制备莪术醇长循环脂质体,对其形态、粒径和电位分布,包封率,体外释放和放置稳定性测定,并考察体外细胞摄取和细胞毒性。结果:制备得到的莪术醇长循环脂质体粒径为(150.3±4.0) nm,PDI为0.197±0.009,zeta电位(-24.5±0.7) mV。莪术醇长循环脂质体平均包封率为80.24%,在4 ℃条件下存放2个月粒径和含药量无明显变化。细胞摄取实验中载香豆素-6长循环脂质体可增强MDA-MB231细胞的摄取。莪术醇长循环脂质体对MDA-MB231细胞具有较强细胞毒性作用,且作用强于莪术醇普通脂质体和游离莪术醇。结论:制备的莪术醇长循环脂质体包封率高,稳定性好,莪术醇长循环脂质体可增强乳腺癌MDA-MB231细胞的摄取及体外细胞毒性。

Preparation and Anti-Breast Cancer Effect of Curcumol PEGylated Liposomes in Vitro

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.