We report a physiologically stable and cytocompatible glucose-responsive nonviral gene delivery system made up of boronate functionalized polymeric material. Herein, we utilize boronate cis-diol interactions to develop a glucose-responsive submicron particle (SMP) system. The stability of the boronate interaction at a physiological pH was achieved by copolymerization of dimethyl aminoethyl methacrylate (DMAEMA) with acrylamidophenylboronic acid (AAPBA) and the formation of a complex with polyvinylalcohol (PVA) which is governed by cis-diol interactions. The shift in hydrodynamic diameter of SMPs was observed and correlated with increasing glucose concentrations at a physiological pH. Optimal transfection was observed for a 5 µg dose of the gaussia luciferase reporter gene in NIH3T3 cells without any adverse effect on cellular viability. The destabilization of the AAPBA–PVA complex by interacting with glucose allowed the release of encapsulated bovine serum albumin (BSA) in a glucose-responsive manner. In total, 95% of BSA was released from SMPs at a 50 mM glucose concentration after 72 h. A two-fold increase in transfection was observed in 50 mM glucose compared to that of 10 mM glucose.

中文翻译：

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通过一锅反应合成的叔胺稳定的硼酸酯-PVA颗粒在生理pH下传递葡萄糖反应性基因

我们报告了由硼酸盐官能化的高分子材料组成的生理稳定和细胞相容性葡萄糖反应性非病毒基因传递系统。在本文中，我们利用硼酸酯顺式-二醇相互作用来开发葡萄糖反应性亚微米颗粒（SMP）系统。硼酸相互作用在生理pH值下的稳定性是通过甲基丙烯酸二甲基氨基乙酯（DMAEMA）与丙烯酰胺基苯基硼酸（AAPBA）的共聚反应以及与聚乙烯醇（PVA）的络合物的形成来实现的，该络合物由顺式控制-二醇相互作用。观察到SMP的流体动力学直径的变化，并且与生理pH下葡萄糖浓度增加相关。在NIH3T3细胞中观察到最佳剂量的5 µg高斯荧光素酶报告基因转染，而对细胞活力没有任何不利影响。通过与葡萄糖相互作用而使AAPBA-PVA复合物失稳，从而使被包封的牛血清白蛋白（BSA）以葡萄糖响应方式释放。总共72小时后，以50 mM葡萄糖浓度从SMP中释放了95％的BSA。与10 mM葡萄糖相比，在50 mM葡萄糖中观察到转染增加了两倍。