Sulfated Glycosaminoglycan-Based Block Copolymer: Preparation of Biocompatible Chondroitin Sulfate-b-poly(lactic acid) Micelles

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• 作者：Andr茅 R. Fajardo ; Alexandre Guerry ; Elizandra A. Britta ; Celso V. Nakamura ; Edvani C. Muniz ; Redouane Borsali ; Sami Halila
• 刊名：Biomacromolecules
• 出版年：2014
• 出版时间：July 14, 2014
• 年：2014
• 卷：15
• 期：7
• 页码：2691-2700
• 全文大小：647K
• ISSN：1526-4602

文摘

Despite a growing interest in amphiphilic polysaccharide-based diblock copolymers as functional polymeric drug delivery nanosystems, biologically relevant sulfated glycosaminoglycan systems were not yet investigated. Here, we report the synthesis and the self-assembly properties in water of chondroitin sulfate-b-poly(lactic acid) (CS-b-PLA_n). The CS-b-PLA_n were synthesized using click-grafting onto method implying reducing-end alkynation of low-molecular weight depolymerized CS (M_w = 5000 g路mol^鈥?) and azide-terminated functionalization of PLA_n (M_w = 6500 g路mol^鈥? (n = 46) and M_w = 1700 g路mol^鈥? (n = 20)). The diblock copolymer self-assembled in water giving rise to spherical micelles that were characterized in solution using dynamic/static light scattering and at dry state by TEM technique. In vitro assays on healthy cells showed that at high concentrations, up to 10 渭g路mL^鈥?, CS-b-PLA_n were noncytotoxic. Those preliminary studies are promising in the perspective to use them as biocompatible nanovehicles for anticancer drug delivery.