论文部分内容阅读
采用单因素试验和正交设计,以包封率为评价指标优化卡培他滨(1)-奥沙利铂(2)复方脂质体的制备方法和处方。采用葡聚糖凝胶微柱分离脂质体与游离药物,高效液相色谱法同时测定2种药物的含量。结果表明,采用薄膜分散法,在药脂比为1∶15、1与2质量比为10∶1、磷脂与胆固醇之比为3∶1和磷脂浓度为8 g/L的条件下可制得平均粒径为199.1 nm、1和2平均包封率为59.8%和52.6%的复方脂质体。体外细胞毒性试验结果表明,1与2质量比不同的脂质体中,比例为15∶1的复方脂质体抑制人肝癌SMMC-7721细胞生长的作用最强,且效果优于剂量更高的1脂质体或2脂质体。
Single factor experiments and orthogonal design were used to optimize the preparation method and prescription of capecitabine (1) - oxaliplatin (2) liposomes with the entrapment efficiency as evaluation index. The liposomes and free drugs were separated by Sephadex micro-column, and the contents of two drugs were determined simultaneously by high performance liquid chromatography. The results showed that under the condition of lipid-lipid ratio 1:15, 1 and 2 mass ratio 10:1, phospholipid-cholesterol ratio 3:1 and phospholipid concentration 8 g / L, The average particle size was 199.1 nm, and the average encapsulation efficiencies of 1 and 2 were 59.8% and 52.6%. In vitro cytotoxicity test results showed that the compound liposomes with the ratio of 1: 2 had the strongest inhibitory effect on the growth of human hepatocellular carcinoma SMMC-7721 cells, and the effect was better than that of the higher dose 1 liposomes or 2 liposomes.