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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 chromatogra-phy,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。
OBJECTIVE: To study the tissue distribution of docetaxel liposomes modified with galactose ligand (Gal-DOC-L) in mice and to investigate the effect of Gal-DOC-L on liver targeting effect. Methods: The concentration of docetaxel in each tissue was determined by high performance liquid chromatogra-phy (HPLC), and compared with docetaxel liposomes (DOC-L) The relative uptake rate re, peak concentration ratio Ce, and targeting efficiency te were used as evaluation parameters to evaluate the liver targeting of Gal-DOC-L. Results: The re of DOC-L and Gal-DOC-L were 2.80 and 4.34, respectively, Ce was 1.67 and 2.38 respectively, te was 28.44% and 38.91% respectively. Conclusion: The drug encapsulated by liposome has a certain target effect on the liver, and the introduction of galactose ligand can further enhance the liposome targeting of the liver.