一种具有肝细胞选择性的脂质体的导向性评价

Targeting Property Evaluation of a Liposome With Specificity to Hepatocyte

目的在细胞水平和小鼠体内评价一种新型脂质体对肝细胞的导向活性。方法采用薄膜水化法制备脂质体,用透射电镜与动态光散射法测定其粒径及分布情况;以脂质体转染荧光素酶质粒的活性以及受体竞争抑制实验,评价脂质体对肝细胞的导向性;以荧光素钠作为报告分子,检测脂质体在小鼠体内的分布及消除情况。结果制备的脂质体为均匀的乳浊状胶体溶液,平均粒径为(103.1±15.3)nm。导向脂质体对肝细胞的转染活性显著高于(P<0.01)普通脂质体,且该转染活性可被半乳糖抑制。导向脂质体可以明显减慢荧光素钠在小鼠体内的吸收与消除的过程,并明显提高荧光素钠在肝组织中的分布含量。结论本实验制备的脂质体在细胞水平与小鼠体内均表现出显著的肝细胞导向性。

Aim To evaluate the targeting property of a liposome with specificity to hepatocyte. Methods liposome was prepared by thin-film hydration method. And theits particle size and distribution were tested by electro microscopy and dynamic light scatter. The specificity of the liposome to hepatocyte was evaluated by plasmid transfection activity and receptor competitive inhibitory effects. With fluorescin as reporter molecules, the distribution and elimination of the liposome were tested in vivo in mice. Results The liposome was homogeneous colloidal solution with an average particle size of （ 103.1 ± 15.3）nm. The targeting liposome had a significantly higher transfection activity to hepatocyte than a common liposome, and this transfection activity can be inhibited by galactose. The targeting liposome can slow down the absorp- tion and elimination of the fluorescin in mice and significantly increase the distribution ratio of fluorescin in liver tissues. Conclusion The targeting liposome prepared in this study showed a prominent hepatocyte targeting property.