胡桃醌叶酸修饰自微乳的体内外靶向性研究  

Study on targeting capacity of Juglone folate modified self-microemulsion in vivo and in vitro

作　　者：黄可心[1] 王晓扬 沈韵桐 李鑫[1] 

机构地区：[1]中国哈尔滨商业大学药学院,黑龙江哈尔滨150076 [2]北京修正创新药物研究院有限公司,北京102209

出　　处：《中国医院药学杂志》2016年第4期285-289,共5页Chinese Journal of Hospital Pharmacy

基　　金：哈尔滨商业大学研究生创新科研项目(编号:YJSCX2014-335HSD)

摘　　要：目的:研究胡桃醌叶酸修饰自微乳在动物体内外的靶向性。方法:(1)采用含体积分数为10%的胎牛血清RPMI-1640培养液,将人胃癌细胞SGC-7901接种到细胞培养瓶中,置于条件为温度37℃,5%CO2浓度培养箱中进行培养。每3天传代一次,取其对数期细胞进行体外各项试验指标的测定。(2)取小鼠分别灌胃各组制剂,分别在给药后0.25,1,4 h将小鼠断头处死,解剖取出心、肝、脾、肺、肾组织和肿瘤组织,采用高效液相色谱法测定各时间点、各器官的药物浓度。结果:(1)结果表明FA-PEG修饰自微乳对胃癌细胞SGC-7901具有明显的体外靶向特征。(2)胡桃醌叶酸修饰自微乳在肿瘤内的药物分布明显高于胡桃醌溶液组和普通自微乳组,在肝内的蓄积量明显低于普通自微乳组,且肿瘤靶向效果最好。结论:胡桃醌叶酸修饰自微乳具有明显的体内外靶向性。ORJECTIVE To study targeting capacity of juglone folate modified self-mieroemulsion in animals. METHODS Human gastric cancer cells SGC-7901 were inoculated into a cell culture flask with RPMI-1640 solution containing 10% fetal bovine,and incubated in 5% CO2 at 37 ℃. For every three days ceils were passaged and logarithmic phase ceils were measured in vitro. Mice were garaged with three preparations, and executed by decollation at 0. 25,1 and 4 h after dosing to collect heart, liver, spleen, lung, kidney and tumor tissues, measure drug concentrations by high performance liquid chromatography. RE- SULTS FA-PEG modified self-mieroemulsion had obvious targeting capacity on gastric cancer cell SGC-7901 in vitro. Juglone folate modified self-microemulsion group had significantly higher drug distribution in tumor than in juglone solution and other ordinary self-microemulsion groups, and significantly lower liver accumulation than in self-microemulsion group. CONCLU- SION Juglone folate modified self-micromulision has obvious targeting in vivo and vitro.

关 键 词：胡桃醌 叶酸 自微乳 靶向性 

分 类 号：R934[医药卫生—生药学]