目的 研究脂质体镶囊的体内分布及载药后的体外药效。 方法 运用共沉淀法和层层自组装技术将Cyanine5标记的牛血清白蛋白（Cy5-BSA）包裹在脂质体镶囊的内部，得到荧光标记的脂质体镶囊Cy5-Capsosome；裸鼠尾静脉注射Cy5-Capsosome，利用活体成像系统观察不同时间点其在裸鼠体内的分布情况；采用四甲基偶氮唑盐微量酶反应比色法（MTT）和细胞凋亡实验考查载多柔比星脂质体镶囊对B16F10细胞的细胞毒性和诱导凋亡的能力。结果 Cy5-Capsosome注射后1 h内即到达肺部，并在肺部蓄积，至少滞留12 h，在其他脏器的分布很少；空白脂质体镶囊细胞毒性较低，载多柔比星脂质体镶囊能明显抑制细胞的生长及诱导细胞的凋亡。 结论 脂质体镶囊具有良好的肺被动靶向性，且具备作为药物载体的潜力。
Abstract
OBJECTIVE To study the tissue distribution of capsosomes in vivo and the efficacy of DOX-loaded capsosomes in vitro.METHODS Cy5-Capsosomes (capsosomes encapsulating Cy5-BSA molecules) were prepared by co-precipitation method and layer-by-layer assembly technique. After intravenously injected into nude mice via the tail vein， the tissue distribution of Cy5-capsosomes at defined time points were studied under Maestro in-vivo imaging system. The cytotoxicity of DOX-loaded capsosomes for B16F10 cells was identified by MTT， the apoptosis induced by DOX-loaded capsosomes was observed by means of fluorescent microscopy. RESULTS Cy5-Capsosomes achieved in the lung less than 1 h and accumulated there for more than 12 h. There was little Cy5-Capsosomes distributed in other organs.Capsosomes had low toxicity， while the DOX-loaded capsosomes had strong toxicity for B16F10 cells and induced apoptosis obviously.CONCLUSION The capsosome had favourable passive pulmonary targetability， and it can be used as a novel drug carrier in potential.
关键词
脂质体镶囊 /
体内分布 /
细胞毒性 /
多柔比星
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Key words
capsosome /
tissue distribution /
cytotoxicity /
doxorubicin
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中图分类号：
R944
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参考文献
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