文獻：Receptor-Specific Delivery of Liposomes Via Folate-Peg-Chol

作者：Wenjin Guo,Tina Lee,Jennifer Sudimack &Robert J. Lee

文獻鏈接：https://www.tandfonline.com/doi/abs/10.3109/08982100009029385

摘要：

A novel lipophilic conjugate of folate, folate-PEG-Chol, was synthesized and evaluated for receptor-mediated targeting of liposomes to tumor cells. Liposomes composed of DSPC/Chol/PEG-DSPE/folate-PEG-Chol (60/ 34/5/1, m/m) were taken up by cultured folate receptor-bearing KB cells via a saturable mechanism. Cellular binding of these liposomes could be competitively inhibited by free folic acid with an IC50 of 0.39 mM, indicating an extraordinarily high binding affinity. Fluorescence micrographs of KB cells treated with targeted liposomes encapsulating calcein showed that they were distributed both on the cell surface and in intracellular vesicular compartments. Targeted liposomes carrying doxorubicin were shown to be 38 times more toxic to KB cells than non-targeted control liposomes. A biodistribution study in receptor-positive tumor-bearing C57BL/6 mice showed no significant differences between the tumor uptake of folate-PEG-liposomes and non-targeted control liposomes. This study has demonstrated that cholesterol could be used as an alternative to phospholipids as an effective anchor for incorporation of a targeting ligand into liposomes.

合成了一種新型的葉酸親脂性綴合物葉酸-PEG-Chol，并評估了其受體介導的脂質體靶向腫瘤細胞的作用。

由DSPC/Chol/PEG-DSPE/葉酸-PEG-Chol（60/34/5/1，m/m）組成的脂質體通過可飽和機制被培養的攜帶葉酸受體的KB細胞吸收。游離葉酸可以競爭性地抑制這些脂質體的細胞結合，IC50為0.39 mM，表明其結合親和力高。

用包封鈣黃綠素的靶向脂質體處理的KB細胞的熒光顯微照片顯示，它們分布在細胞表面和細胞內囊泡隔室中。攜帶阿霉素的靶向脂質體對KB細胞的毒性是非靶向對照脂質體的38倍。

在受體陽性腫瘤攜帶C57BL/6小鼠中的生物分布研究表明，葉酸-PEG脂質體和非靶向對照脂質體的腫瘤攝取之間沒有顯著差異。這項研究表明，膽固醇可以作為磷脂的替代品，作為將靶向配體摻入脂質體的有效錨。

相關推薦：

DPPE-PEG-BIOTIN

DPPE-PEG-COOH

DPPE-PEG-Mal

DPPE-PEG-N3

DPPE-PEG-NH2

DPPE-PEG-SC

DSPE(Sodium salt)-PEG-COOH

DSPE(Sodium salt)-PEG-NH2

DSPE(Sodium salt)-PEG-OH

DLPE-PEG-COOH

DLPE-PEG-Mal

DLPE-PEG-NH2

DLPE-PEG-SC

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