维生素A-姜黄素脂质体的制备及细胞毒性研究  

Study on Preparation of Vitamin A-Curcumin Liposome and Its Cytotoxicity

作　　者：孟路华[1] 赵怡[1] 潘黎军[1] 王驰[1] 

机构地区：[1]重庆医科大学药学院,重庆400016

出　　处：《中国药学杂志》2011年第14期1104-1107,共4页Chinese Pharmaceutical Journal

摘　　要：目的制备肝星状细胞靶向维生素A-姜黄素脂质体(VA-CUR-L),并进行体外细胞毒性实验。方法采用逆相蒸发法制备VA-CUR-L,测定其包封率及VA结合率;脂质体分别在4,25℃下密闭放置30 d,以包封率、VA结合率及过氧化值为指标考察其稳定性;以视黄醇结合蛋白受体高表达的鼠肝星状细胞HSC-T6和无视黄醇结合蛋白受体表达的人食管癌细胞A-549为细胞模型,采用MTT法考察该脂质体的细胞毒性及靶向性。结果脂质体平均包封率为89.32%,VA结合率为61.34%;脂质体于4℃贮存较稳定;细胞实验显示,游离姜黄素、姜黄素脂质体及VA-CUR-L对HSC-T6的IC50值分别为31.53,14.95和8.28μg·mL-1,姜黄素脂质体和VA-CUR-L对A-549细胞作用相当。结论 在最佳工艺条件下制得的VA-CUR-L包封率高、稳定性好,且可特异性靶向作用于肝星状细胞,提高药物疗效。OBJECTIVE To prepare Hepatic stellate cell targeting Vitamin A-curcumin liposome and to investigate its cytotoxicity in vitro.METHODS Reverse phase evaporation was used to prepare VA-curcumin liposome and the entrapment efficiency and the VA binding rate was determined.Entrapment efficiency,VA binging rate and peroxide value were determined to evaluate the stability of liposome at 4 and 25 ℃ for 30 d.MTT assay was used to investigate the cytotoxicity and targeting ability of the liposome in rat hepatic stellate cells HSC-T6 with high expression of retinol binding protein and human esophageal cancer cells A-549 without expression of retinol binding protein.RESULTS The average entrapment efficiency for curcumin was 89.32%,and binding rate for VA was 61.34%.The liposome stored at 4 ℃ was stable.The results of MTT assay showed that IC50 of curcumin,curcumin liposome,and VA-curcumin liposome in HSC-T6 cell were 31.53,14.95 and 8.28 μg·mL-1,respectively.Curcumin liposome and VA-curcumin liposome had same cytotoxic effects in A-549 cell.CONCLUSION The optimized conditions were obtained with high entrapment efficiency and good stability.VA-curcumin liposome could specifically target HSC and promote therapeutic effect of curcumin.

关 键 词：肝星状细胞 姜黄素 维生素A 脂质体 细胞毒作用 靶向性 

分 类 号：R944[医药卫生—药剂学]