文章摘要
吴 卫,程 怡,吴 琼.半乳糖配体介导多烯紫杉醇脂质体靶向性研究[J].南京医科大学学报,2012,(2):168~171
半乳糖配体介导多烯紫杉醇脂质体靶向性研究
A targetability study of docetaxel liposomes mediated with galactose ligand
投稿时间:2011-10-08  
DOI:10.7655
中文关键词: 多烯紫杉醇  脂质体  半乳糖配体  靶向给药
英文关键词: docetaxel  liposomes  asialoglycoprotein receptor  targeted drug delivery
基金项目:国家自然科学基金资助项目(30772790)
作者单位
吴 卫 广州中医药大学中药学院,广东 广州 510006/桂林医学院药学院,广西 桂林 541004 
程 怡 广州中医药大学中药学院,广东 广州 510006 
吴 琼 广州中医药大学中药学院,广东 广州 510006 
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中文摘要:
      目的:研究经半乳糖配体修饰后的多烯紫杉醇脂质体(docetaxel liposomes modified with galactose ligand,Gal-DOC-L)在小鼠体内的组织分布,探讨Gal-DOC-L对肝脏的靶向作用?方法:采用高效液相色谱法(high performance liquid chromatography,HPLC)测定各组织中多烯紫杉醇的药物浓度,以多烯紫杉醇普通脂质体(docetaxel liposomes,DOC-L)为对比,分别采用相对摄取率re?峰浓度比Ce和靶向效率te作为评价参数,对Gal-DOC-L的肝靶向性进行评价?结果:DOC-L和Gal-DOC-L的re分别为2.80和4.34,Ce分别为1.67和2.38,te分别为28.44%和38.91%?结论:药物经脂质体包封后对肝脏具有一定的靶向效应,而半乳糖配体的引入可进一步提高脂质体对肝脏的靶向性?
英文摘要:
      Objective: To study the tissue distribution of docetaxel liposomes modified with galactose ligand (Gal-DOC-L) in mice after intravenous injection,and to discuss the liver targeted effects of Gal-DOC-L. Methods: The determination of drug tissue distribution in mice was measured by HPLC,relative uptake rate (re),peak concentration ratio (Ce) and targeting efficiency (te) were used as the evaluation parameters to evaluate the DOC-L,Gal-DOC-L’s liver targeted effect. Results: The relative uptake rates of DOC-L and Gal-DOC-L were 2.80 and 4.34,peak concentration ratios of DOC-L and Gal-DOC-L were 1.67 and 2.38,targeting efficiency percentages of DOC-L and Gal-DOC-L were 28.44% and 38.91%. Conclusion: The drug encapsulated by liposomes has a certain effect of targetability,and liposomes modified with galactose ligand-targeted could further improve the hepatic targeted effect.
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