Key Laboratory of Hormones and Development Ministry of Health, Metabolic Diseases Hospital, Tianjin Medical University, Tianjin 300070, China.
J Pharm Sci. 2011 Jun;100(6):2278-86. doi: 10.1002/jps.22463. Epub 2011 Jan 25.
To develop self-regulated insulin delivery system, the glucose-sensitive copolymers with a fraction of phenylboronic acid group were prepared by the coupling reaction of -COOH of N-(carboxyacyl) chitosan and -NH(2) of 3-aminophenylboronic acid. A sufficient glucose sensitivity of the copolymer was accomplished by the glucose-induced volume changes of the nanoparticles and release profiles of insulin in phosphate buffered saline (PBS, pH 7.4) with different glucose concentrations, which occurred in a remarkable glucose concentration-dependent manner. Furthermore, circular dichroism spectroscopy demonstrates that the overall tertiary structure of the released insulin was not altered compared with that of the standard insulin. The analysis of relative cell proliferation suggests that the copolymer showed good cytocompatibility. The glucose-sensitive copolymers have a potential use in self-regulated drug-releasing systems.
为了开发自我调节的胰岛素输送系统，通过 N-（羧基酰基）壳聚糖的-COOH 和 3-氨基苯硼酸的-NH2 的偶联反应，制备了具有部分苯硼酸基团的葡萄糖敏感共聚物。通过纳米粒子的葡萄糖诱导的体积变化和在不同葡萄糖浓度的磷酸盐缓冲盐水（PBS，pH7.4）中的胰岛素释放曲线，实现了共聚物的充分葡萄糖敏感性，其显著地依赖于葡萄糖浓度。此外，圆二色性光谱表明，与标准胰岛素相比，释放的胰岛素的整体三级结构没有改变。相对细胞增殖的分析表明，共聚物具有良好的细胞相容性。葡萄糖敏感共聚物在自我调节药物释放系统中有潜在的应用。
