论文部分内容阅读
采用硫酸铵梯度法制得了平均粒径为(45.3±12.6)nm、包封率为(93.8±0.7)%的盐酸伊立替康脂质体。制品在pH7.4磷酸盐缓冲液中约120 h释放完全,提示其具有缓释作用。体外细胞毒性试验显示,制品在较高浓度(25 g/ml以上)对人结肠癌细胞株HT-29的抑制作用稍优于游离药物,IC50分别为28.1和33.0 g/ml。细胞凋亡试验表明,30 g/ml的脂质体和游离药物均能诱导HT-29细胞的凋亡,与游离药物相比,脂质体具有更强的凋亡诱导效果。
The irinotecan hydrochloride liposomes with mean diameter of (45.3 ± 12.6) nm and entrapment efficiency of (93.8 ± 0.7)% were obtained by ammonium sulfate gradient method. The product was completely released in pH7.4 phosphate buffer for about 120 h, suggesting that it has a sustained release effect. In vitro cytotoxicity tests showed that the inhibitory effect of the product at a higher concentration (above 25 g / ml) on human colon cancer cell line HT-29 was slightly better than that of the free drug with IC50 values of 28.1 and 33.0 g / ml, respectively. Apoptosis assay showed that both liposome and free drug at 30 g / ml could induce apoptosis of HT-29 cells, and the liposomes had stronger apoptosis-inducing effect than free drug.