文獻(xiàn)：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

文獻(xiàn)鏈接：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.

開(kāi)發(fā)了一種新技術(shù)，用于形成可適用于各種配體的配體靶向聚合物膠束。對(duì)于腫瘤特異性藥物遞送，負(fù)載喜樹(shù)堿（CPT）的聚合物膠束被葉酸修飾，產(chǎn)生葉酸受體靶向藥物載體。

當(dāng)制備負(fù)載藥物的聚合物膠束時(shí)，加入葉酸連接的PEG5000二硬脂酰磷脂酰乙醇胺（Folate-PEG5000-DSPE），導(dǎo)致葉酸配體暴露在表面。通過(guò)使用流式細(xì)胞儀、熒光顯微鏡和共聚焦激光掃描顯微鏡測(cè)量細(xì)胞攝取以及細(xì)胞毒性測(cè)量來(lái)評(píng)估葉酸修飾的CPT負(fù)載聚合物膠束（F-膠束）。

結(jié)果表明，與KB細(xì)胞中未經(jīng)葉酸修飾的CPT負(fù)載聚合物膠束（普通膠束）相比，F(xiàn)-膠束在過(guò)表達(dá)葉酸受體（FR）的KB細(xì)胞中表現(xiàn)出更高的細(xì)胞攝取率和更高的毒性，但在FR陰性的HepG2細(xì)胞中則不然。

這一結(jié)果表明，葉酸連接的脂質(zhì)成功地修飾了聚合物膠束。

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