采用超声薄膜水化法制备包裹大豆异黄酮主要功能成分染料木黄酮(Ge)的甘露糖修饰聚乙二醇化纳米脂质体(man-PEG@LP/Ge)。伴刀豆球蛋白A(ConA)凝集实验证实甘露糖能够成功修饰在纳米脂质体表面。man-PEG@LP/Ge呈规则的球形, 大小分布均一, 颗粒分散性好。其粒径为(270±15) nm, Zeta电位为+7.5 mV。由于聚乙二醇(PEG)长链的空间位阻效应和颗粒所带正电荷的排斥作用实现了较强的结构刚性和较好的稳定性。流式细胞术的结果表明: man-PEG@LP/Ge能够特异性的识别甘露糖受体高表达的人肝癌Huh-7细胞。细胞毒理实验证明: 药物载体man-PEG@LP本身没有毒副作用, 生物相容性较好。细胞水平和动物水平的肿瘤杀伤实验结果表明: 运载药物之后的man-PEG@LP/Ge在甘露糖介导的“主动靶向”作用下高效而特异性的进入肿瘤细胞, 对肿瘤组织进行了有效地杀伤。

Genistein doped mannose-conjugated PEG-modified liposomes (man-PEG@LP/Ge) were prepared via film-sonic method by using targeted lipid DSPE-PEG-man and helper lipid DOTAP. Concanavalin A (ConA) agglutination assay had proved that mannose has been modified to nano-liposomes successfully. The as-prepared man-PEG@LP/Ge were spherical in shape with a homogeneous size distribution around (270±15) nm in diameter as characterized by SEM. The Zeta potential was +7.5 mV in pure water. Furthermore, man-PEG@LP/Ge appeared to be very homogeneous and stable in water. It is considered that the steric-hinerance effects of surface PEG long chain and the strong electrostatic repulsion of the positive charge play an important role in the good dispersion of man-PEG@LP/Ge. Flow cytometry examination confirmed the targeting specificity of man-PEG@LP/Ge against human hepatoma Huh-7 cells which are of over-expression of mannose receptors. The cell toxicity viability demonstrated that unloaded man-PEG@LP are practically non-toxic, indicating that the drug delivery vehicles possess excellent biocompatibility. Systematic in vitro and in vivo studies showed that the man-PEG@LP/Ge kill tumor cells with high specificity and excellent efficiency, owing to the mannose-mediated active tumor-targeted drug delivery.