Synthesis and In Vitro Cancer Cell Targeting of Folate-Functionalized Biodegradable Amphiphilic Dendrimer-Like Star Polymers

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• 作者：Weiqiang Cao ; Jing Zhou ; Yong Wang ; Lei Zhu
• 刊名：Biomacromolecules
• 出版年：2010
• 出版时间：December 13, 2010
• 年：2010
• 卷：11
• 期：12
• 页码：3680-3687
• 全文大小：550K
• 年卷期：v.11,no.12(December 13, 2010)
• ISSN：1526-4602

文摘

By coupling a well-defined PLLA star polymer with six carboxylic acid-terminated polyester dendrons based on 2,2-bis(hydroxymethyl)propionic acid, a biodegradable dendrimer-like star polymer (DLSP) with multiple carboxylic acid groups at the outer surface was successfully synthesized. Conjugation of amine-functionalized folic acids (FA) onto the DLSP yielded a folate-DLSP hybrid as a carrier for targeted drug delivery. The chemical structures were proven by proton nuclear magnetic resonance and size exclusion chromatography. The DLSPs could form unimolecular micelles with a mean particle size of about 18 nm, as determined by dynamic light scattering. Flow cytometry and confocal microscope studies revealed that the cellular uptake of the folate-DLSP hybrid against KB cells (overexpressed folate-receptor) was much higher than that of the neat DLSP (without FA) due to the folate receptor-mediated binding.