文献：Polymeric Micelles Modified by Folate-PEG-Lipid for Targeted Drug Delivery to Cancer Cells In Vitro

作者： Hayama, Akihiro; Yamamoto, Tatsuhiro; Yokoyama, Masayuki; Kawano, Kumi; Hattori, Yoshiyuki; Maitani, Yoshie

文献链接：https://www.ingentaconnect.com/contentone/asp/jnn/2008/00000008/00000006/art00040

摘要：

A novel technique was developed for the formation of ligand-targeted polymeric micelles that can be applicable to various ligands. For tumor-specific drug delivery, camptothecin (CPT)-loaded polymeric micelles were modified by folate to produce a folate-receptor-targeted drug carrier. Folate-linked PEG5000-distearoylphosphatidylethanolamine (folate-PEG5000-DSPE) was added when preparations of drug-loaded polymeric micelles, resulting in folate ligands exposed to the surface. Folate-modified CPT-loaded polymeric micelles (F-micelle) were evaluated by measuring cellular uptake using a flow cytometer, fluorescence microscopy, and confocal laser scanning microscopy, and by cytotoxicity measurement. The results revealed that F-micelle showed higher cellular uptake in KB cells over-expressing folate receptor (FR) and higher cytotoxicity compared with non-folate modified CPT-loaded polymeric micelles (plain micelles) in KB cells, but not in FR-negative HepG2 cells. This result indicated that polymeric micelles were successfully modified by the folate-linked lipid.

开发了一种新技术，用于形成可适用于各种配体的配体靶向聚合物胶束。对于肿瘤特异性药物递送，负载喜树碱（CPT）的聚合物胶束被叶酸修饰，产生叶酸受体靶向药物载体。

当制备负载药物的聚合物胶束时，加入叶酸连接的PEG5000二硬脂酰磷脂酰乙醇胺（Folate-PEG5000-DSPE），导致叶酸配体暴露在表面。通过使用流式细胞仪、荧光显微镜和共聚焦激光扫描显微镜测量细胞摄取以及细胞毒性测量来评估叶酸修饰的CPT负载聚合物胶束（F-胶束）。

结果表明，与KB细胞中未经叶酸修饰的CPT负载聚合物胶束（普通胶束）相比，F-胶束在过表达叶酸受体（FR）的KB细胞中表现出更高的细胞摄取率和更高的毒性，但在FR阴性的HepG2细胞中则不然。

这一结果表明，叶酸连接的脂质成功地修饰了聚合物胶束。

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DSPE-PEG-Alkyne

DSPE-PEG-Rhodamine

DSPE-Rhodamine

DSPE-PEG-SH

DSPE-PEG-SPDP

DSPE-SPDP

DSPE-PEG-TFP

DSPE-PEG13-TFP

DSPE-PEG-Vinylsulfone

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