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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 cells targeting vitamin A-curcumin liposomes (VA-CUR-L) and to conduct in vitro cytotoxicity experiments. Methods VA-CUR-L was prepared by reverse phase evaporation method. The entrapment efficiency and VA binding rate were determined. The liposomes were placed in confinement at 4 and 25 ℃ for 30 days respectively. The entrapment efficiency, VA binding rate and peroxide value As the index to investigate the stability of HSC-T6. The human esophageal carcinoma cell line A-549, which is a high expression of retinol binding protein receptor, was used as the cell model. MTT assay The liposomes were investigated for cytotoxicity and targeting. RESULTS: The average entrapment efficiency of liposomes was 89.32% and the VA binding rate was 61.34%. The liposomes were stable at 4 ℃. The results of cell experiments showed that free curcumin, curcumin liposomes and VA-CUR- The IC50 values of -T6 were 31.53, 14.95 and 8.28μg · mL-1, respectively. Curcumin liposomes and VA-CUR-L had the same effect on A-549 cells. CONCLUSION VA-CUR-L prepared under optimal conditions has high encapsulation efficiency and good stability, and can be specifically targeted to hepatic stellate cells to improve the efficacy of the drug.