中国临床药理学与治疗学2017，Vol.22Issue(11)：1207-1214,8.
紫杉醇聚合物胶束的组织分布和生物学评价
Biodistribution and biological evaluation of paclitaxel polymer micelles
摘要
Abstract
AIM:The biodistribution in tumorbearing mice and biosafety of paclitaxel (FTX) polymer micelles were investigated.METHODS:The pharmacokinetic study,tissue distribution and antineoplastic effect of PTX polymer micelles and Taxol were evaluated on S180 tumor-bearing mice after intravenous injection.Animals were used to research the acute toxicity,hemolysis and venous irritation of PTX polymer micelle.RESULTS:The t1/2 and MRT of PTX polymer micelles were 3.52 and 4.55 times of Taxol,respectively.Tissue distribution studies showed that the relative uptake rate of PTX polymer micelles at tumor sites was 2.31.The results indicated that PTX polymer micelles improved the circulation time and tumor targeting.The antitumor efficacy of PTX polymer micelles was significantly higher than Taxol.Maximum tolerated dose and LD50 of PTX polymer micelles were significantly improved.PTX polymer micelles had no obvious vascular irritation to ear vein of rabbits.CONCLUSION:The circulation time,tumor targeting,antineoplastic effect and biosafety of FTX polymer micelles were improved,which might turn into a promising tumor targeting paclitaxel polymer micelle preparations in clinic with maximum effect and minmum toxicity.关键词
紫杉醇/聚合物胶束/组织分布/抗肿瘤活性/安全性评价Key words
paclitaxel/polymer micelles/biodistribution/antitumor efficacy/safety study分类
医药卫生引用本文复制引用
姚天怡,尹少平,刘雯,赵炎磊,王广基,李娟..紫杉醇聚合物胶束的组织分布和生物学评价[J].中国临床药理学与治疗学,2017,22(11):1207-1214,8.基金项目
国家自然科学基金面上项目(81373363) （81373363）
国家科技部十一五重大新药创制(2009ZX09310-004) （2009ZX09310-004）
江苏省科技支撑-社会发展项目(BE2010723) （BE2010723）
江苏省研究生创新工程(CXLX11-0813) （CXLX11-0813）
