摘要
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 the mean particle size and entrapment efficiency of （45.3±12.6） nm and （93.8±0.7） % were prepared by ammonium sulfate gradient method. The drug was released completely from the liposomes within 120 h in phosphate buffer （pH 7.4） in a manner of sustained release. Compared with the free drug, the prepared liposomes showed slightly higher in vitro cytotoxicity on human colorectal cancer HT-29 cells at relatively high concentration （above 25μg/ml）. The ICs0 values of the product and free drug were 28.1 and 33.0 ~tg/ml, respectively. Both liposomes and free drug could induce apoptosis of HT-29 cells at the drug concentration of 30μg/ml, but the liposomes exhibited a stronger effect on the induction of cell apoptosis than free drug.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2013年第6期576-580,共5页
Chinese Journal of Pharmaceuticals
关键词
盐酸伊立替康
脂质体
制备
硫酸铵梯度法
体外抗肿瘤活性
irinotecan hydrochloride
liposome
preparation
ammonium sulfate gradient method
in vitro antitumor activity
