文献：Folate-mediated tumor cell targeting of liposome-entrapped doxorubicin in vitro

作者：Robert J Lee, Philip S Low

文献链接：https://www.sciencedirect.com/science/article/pii/000527369400235H

摘要：

Receptors for the vitamin folic acid are frequently overexpressed on epithelial cancer cells. To examine whether this overexpression might be exploited to specifically deliver liposome-encapsulated drug molecules in vitro, folate-targeted liposomes were prepared by incorporating 0.1 mol% of a folate-polyethyleneglycol-distearoylphosphatidylethanolamine (folate-PEG-DSPE) construct into the lipid bilayer, and were loaded with doxorubicin (DOX), an anti-cancer drug. Uptake of folate-PEG-liposomal DOX by KB cells was 45-fold higher than that of non-targeted liposomal DOX, and 1.6-times higher than that of free DOX, while the cytotoxicity was 86 and 2.7-times higher, respectively. Folate-targeting is fully compatible with PEG-coating of the liposomes, since incorporation of 4 mol% PEG2000-DSPE does not reduce the uptake or cytotoxicity of folate-PEG-liposomal DOX. Uptake of folate-PEG-liposomes was inhibited by 1 mM free folic acid but was unaffected by physiological concentrations of folate. In HeLa/W138 co-cultures, folate-PEG-liposomes encapsulating calcein, a fluorescent dye, were found to be almost exclusively internalized by the HeLa cells which overexpress the folate receptors. We suggest that folate targeting constitutes a possible mechanism for improving the specificity of PEG-coated liposomes for cancer cells.

检查这种过度表达是否可用于在体外特异性递送脂质体包裹的药物分子，通过将0.1mol%的叶酸-亚乙基二醇-二硬脂酰磷脂酰乙醇胺（叶酸-PEG-DSPE）构建体掺入脂质双层中制备叶酸靶向脂质体，并负载药物阿霉素（DOX）。

KB细胞对叶酸-PEG脂质体DOX的摄取量比非靶向DOX高45倍，比游离DOX高1.6倍，而细胞毒性分别高86倍和2.7倍。

叶酸靶向与脂质体的PEG涂层完全兼容，因为掺入4 mol%的PEG2000-DSPE不会降低叶酸-PEG脂质体DOX的摄取或细胞毒性。

叶酸-PEG脂质体的摄取受到1mM游离叶酸的抑制，但不受叶酸生理浓度的影响。

在HeLa/W138共培养中，发现包封钙黄绿素（一种荧光染料）的叶酸-PEG脂质体几乎完全被过表达叶酸受体的HeLa细胞内化。

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