硬脂醇半乳糖苷修饰的阿西替尼脂质体的制备及体外活性研究
发布时间：2019-06-21 06:33
【摘要】：目的制备硬脂醇半乳糖苷修饰的阿西替尼脂质体,并进行处方筛选及体外活性研究。方法采用硫酸铵梯度法制备硬脂醇半乳糖苷修饰的阿西替尼脂质体,以包封率及粒径为评价指标,采用Box-Behnken响应面设计法优化制备工艺,并研究硬脂醇半乳糖苷修饰的阿西替尼脂质体对人肝癌SMMC-7721细胞株的增殖抑制及凋亡的诱导作用。采用CCK-8法检测硬脂醇半乳糖苷修饰的阿西替尼脂质体对人肝癌SMMC-7721细胞株的生长抑制情况,采用了Annexin V/PI流式细胞分析法检测细胞凋亡。结果最佳工艺:药与磷脂比为1∶14.95,胆固醇与磷脂之比为1∶4.45,水浴温度为61.93℃,硫酸铵溶液的体积为4.31 m L。硬脂醇半乳糖苷修饰的阿西替尼脂质体的粒径为(252±6.4)nm,包封率为(68.50±0.85)%。CCK-8细胞毒性试验结果显示,在药物浓度相同时,抑制率随时间的延长而增加;作用时间相同时,抑制率随药物浓度的增大而增加。Annexin V/PI流式试验结果显示,硬脂醇半乳糖苷修饰的阿西替尼脂质体对人肝癌SMMC-7721细胞株的抑制率优于人肝癌A549细胞株。结论硫酸铵梯度法制备硬脂醇半乳糖苷修饰的阿西替尼脂质体的处方合理,工艺可行,包封率高。硬脂醇半乳糖苷修饰的阿西替尼脂质体对人肝癌SMMC-7721细胞株有更高的细胞毒性,诱导SMMC-7721细胞株凋亡能力比A549的强。初步判定硬脂醇半乳糖苷修饰的阿西替尼脂质体具有主动肝靶向性。
[Abstract]:Objective to prepare stearol galactoside modified acitinib liposomes and to study the prescription screening and in vitro activity of acitinib liposomes. Methods Azetinib liposomes modified by stearyl galactoside were prepared by ammonium sulfate gradient method. The encapsulation efficiency and particle size were used as evaluation indexes. Box-Behnken response surface design was used to optimize the preparation process, and the effect of stearyl galactoside modified acitinib liposomes on proliferation and apoptosis of human hepatocellular carcinoma SMMC-7721 cell line was studied. CCK-8 assay was used to detect the inhibitory effect of stearyl galactoside modified azetinib liposomes on the growth of human hepatocellular carcinoma SMMC-7721 cell line, and Annexin V/PI flow cytometry was used to detect apoptosis. Results the optimum conditions were as follows: the ratio of drug to phospholipid was 1 鈮，
本文编号：2503868
[Abstract]:Objective to prepare stearol galactoside modified acitinib liposomes and to study the prescription screening and in vitro activity of acitinib liposomes. Methods Azetinib liposomes modified by stearyl galactoside were prepared by ammonium sulfate gradient method. The encapsulation efficiency and particle size were used as evaluation indexes. Box-Behnken response surface design was used to optimize the preparation process, and the effect of stearyl galactoside modified acitinib liposomes on proliferation and apoptosis of human hepatocellular carcinoma SMMC-7721 cell line was studied. CCK-8 assay was used to detect the inhibitory effect of stearyl galactoside modified azetinib liposomes on the growth of human hepatocellular carcinoma SMMC-7721 cell line, and Annexin V/PI flow cytometry was used to detect apoptosis. Results the optimum conditions were as follows: the ratio of drug to phospholipid was 1 鈮，
本文编号：2503868
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