Zhang Yu-Hui, Zhang Ying-Ming, Zhao Qi-Hui, Liu Yu
Department of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071 P. R. China.
Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Nankai University, Tianjin 300071 P. R. China.
Sci Rep. 2016 Mar 7;6:22654. doi: 10.1038/srep22654.
Drug/gene transportation systems with stimuli-responsive release behaviors are becoming research hotspots in biochemical and biomedical fields. In this work, a glucose-responsive supramolecular nanocluster was successfully constructed by the intermolecular complexation of phenylboronic acid modified β-cyclodextrin with adamantane modified polyethylenimine, which could be used as a biocompatible carrier for insulin and pCMV3-C-GFPSpark-Ins DNA which could express insulin co-delivery. Benefiting from the response capability of phenylboronic acid moiety toward glucose, the encapsulated insulin could be specifically released and the corresponding targeted DNA could efficiently express insulin in HepG2 cell, accompanied by the high-level insulin release in vitro. Our results demonstrate that the simultaneous insulin drug delivery and insulin gene transfection in a controlled mode may have great potential in the clinical diabetes treatments.
具有刺激响应释放行为的药物/基因传输系统正成为生化和生物医学领域的研究热点。在本研究中,通过苯硼酸修饰的β-环糊精与金刚烷修饰的聚乙烯亚胺的分子间络合,成功构建了一种葡萄糖响应性超分子纳米簇,其可作为胰岛素和pCMV3-C-GFPSpark-Ins DNA(可表达胰岛素)共递送的生物相容性载体。受益于苯硼酸部分对葡萄糖的响应能力,包封的胰岛素可被特异性释放,相应的靶向DNA可在HepG2细胞中高效表达胰岛素,同时在体外实现高水平的胰岛素释放。我们的结果表明,以可控方式同时进行胰岛素药物递送和胰岛素基因转染在临床糖尿病治疗中可能具有巨大潜力。