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

作者：Robert J Lee, Philip S Low

文獻鏈接：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.

檢查這種過度表達是否可用于在體外特異性遞送脂質(zhì)體包裹的藥物分子，通過將0.1mol%的葉酸-亞乙基二醇-二硬脂酰磷脂酰乙醇胺（葉酸-PEG-DSPE）構建體摻入脂質(zhì)雙層中制備葉酸靶向脂質(zhì)體，并負載藥物阿霉素（DOX）。

KB細胞對葉酸-PEG脂質(zhì)體DOX的攝取量比非靶向DOX高45倍，比游離DOX高1.6倍，而細胞毒性分別高86倍和2.7倍。

葉酸靶向與脂質(zhì)體的PEG涂層完全兼容，因為摻入4 mol%的PEG2000-DSPE不會降低葉酸-PEG脂質(zhì)體DOX的攝取或細胞毒性。

葉酸-PEG脂質(zhì)體的攝取受到1mM游離葉酸的抑制，但不受葉酸生理濃度的影響。

在HeLa/W138共培養(yǎng)中，發(fā)現(xiàn)包封鈣黃綠素（一種熒光染料）的葉酸-PEG脂質(zhì)體幾乎完全被過表達葉酸受體的HeLa細胞內(nèi)化。

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