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

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

文献链接：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.

合成了一种新型的叶酸亲脂性缀合物叶酸-PEG-Chol，并评估了其受体介导的脂质体靶向肿瘤细胞的作用。

由DSPC/Chol/PEG-DSPE/叶酸-PEG-Chol（60/34/5/1，m/m）组成的脂质体通过可饱和机制被培养的携带叶酸受体的KB细胞吸收。游离叶酸可以竞争性地抑制这些脂质体的细胞结合，IC50为0.39 mM，表明其结合亲和力高。

用包封钙黄绿素的靶向脂质体处理的KB细胞的荧光显微照片显示，它们分布在细胞表面和细胞内囊泡隔室中。携带阿霉素的靶向脂质体对KB细胞的毒性是非靶向对照脂质体的38倍。

在受体阳性肿瘤携带C57BL/6小鼠中的生物分布研究表明，叶酸-PEG脂质体和非靶向对照脂质体的肿瘤摄取之间没有显著差异。这项研究表明，胆固醇可以作为磷脂的替代品，作为将靶向配体掺入脂质体的有效锚。

相关推荐：

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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