Monosaccharide-Responsive Release of Insulin from Polymersomes of Polyboroxole Block Copolymers at Neutral pH
Monosaccharide-Responsive Release of Insulin from Polymersomes of Polyboroxole Block Copolymers at Neutral pH
复制标题
DOI：
10.1021/ja211728x
复制
发表时间：
2012-03-07
影响因子：
15
通讯作者：
Kim, Kyoung Taek
中科院分区：
文献类型：
--
作者：
Kim, Hyunkyu;Kang, Young Ji;Kim, Kyoung Taek
通过可逆加成、裂解和链转移(RAFT)法合成了一种含硼氧烷的苯并烯单体。聚苯乙烯硼氧烷(PBOx)及其与聚乙二醇(PEG)的嵌段共聚物在中性pH的磷酸盐缓冲溶液中与单糖结合，通过Wang的竞争结合实验进行定量。通过可控的自由基聚合，我们能够调节PBOx嵌段的聚合度，以产生糖响应型嵌段共聚物，这些嵌段共聚物自组装成各种纳米结构，包括球形和圆柱形胶束和聚合物小泡(聚合体)。这些嵌段共聚物的聚合体在中性pH介质中表现出单糖响应性拆解。我们证明了在中性磷酸盐缓冲液(pH 7.4)中将这些聚合体用作胰岛素的糖响应性递送载体的可能性。只有在生理相关的pH条件下，糖的存在才能从聚合体中释放包裹的胰岛素。
We synthesized a boroxole-containing styrenic monomer that can be polymerized by the reversible addition fragmentation and chain transfer (RAFT) method. Poly(styreneboroxole) (PBOx) and its block copolymers with a poly(ethylene glycol) (PEG) as a hydrophilic block displayed binding to monosaccharides in phosphate buffer at neutral pH, as quantified by Wang's competitive binding experiments. By virtue of a controlled radical polymerization, we were able to adjust the degree of polymerization of the PBOx block to yield sugar-responsive block copolymers that self-assembled into a variety of nanostructures including spherical and cylindrical micelles and polymer vesicles (polymersomes). Polymersomes of these block copolymers exhibited monosaccharide-responsive disassembly in a neutral-pH medium. We demonstrated the possibility of using these polymersomes as sugar-responsive delivery vehicles for insulin in neutral phosphate buffer (pH 7.4). Encapsulated insulin could be released from the polymersomes only in the presence of sugars under physiologically relevant pH conditions.