雷公藤红素脂质体的制备及体外细胞实验研究

Preparation and Experimental Study of Cells in Vitro of Celastrol Liposomes

目的制备雷公藤红素脂质体并对其体外抗U87 MG肿瘤细胞增殖作用进行研究。方法建立了雷公藤红素脂质体的HPLC分析方法,采用薄膜分散法制备雷公藤红素脂质体,正交实验优化获得最佳处方,并对粒径、Zeta电位、形态及体外释放行为和药效学进行考察。结果雷公藤红素脂质体的体外分析方法简单可行;脂质体最佳处方为:5%的大豆卵磷脂,药脂比为1∶20,磷脂与胆固醇之比为6∶1,水化介质为10%海藻糖溶液。脂质体的粒径为163nm,Zeta电位为-35mv,体外释放实验表明雷公藤红素脂质体具有缓释作用,而且雷公藤红素脂质体的抗U87 MG细胞增殖作用强于游离药物,IC 50为0.0560μg·mL-1。结论雷公藤红素脂质体具有良好的抗U87 MG细胞增殖作用。

OBJECTIVE To prepare cholesterol loaded liposomes and evaluate the cytotoxicity of celastrol liposomes against U87 MG cells in vitro.METH ODS A HPLC method was established in vitro for celastrol determination,celastrol-loaded liposomes were prepared by the thin film-hydration method.Orthogonal experiments were conducted to optimize the prescription.Entrapment efficiency,particle size,zeta potential and the anti-proliferative effects of celastrol-loaded liposomes were evaluated.RESULTS The particle size of celastrol-loaded liposomes was about 163nm with small size distribution.The best optimization prescription was as follows:ratio of drug and lipid was 1∶20,the ratio of phospholipids and cholesterol was 6∶1 with 10%trehalose solvent as hydrationmedium.Release profiles in vitro demonstrated that celastrol-loaded liposomes possessed a preferred release feature.Furthermore,the MTT assay showed that celastrol-loaded liposomes had better anti-proliferative effect to U87MG cells than free celastrol,the IC 50 value of celastrol liposomes was 0.0560μg·mL-1.CONCLUSION Celastrol loaded liposomes have good propertie of antiproliferative effects against U87 MG glioma cells.