Sugar-responsive pseudopolyrotaxanes and their application in sugar-induced release of PEGylated insulin
Sugar-responsive pseudopolyrotaxanes and their application in sugar-induced release of PEGylated insulin
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DOI：
10.1007/s10847-015-0504-0
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发表时间：
2015-03
影响因子：
2.3
通讯作者：
T. Seki;Keigo Abe;Kiminobu Nakamura;Yuya Egawa;R. Miki;K. Juni;T. Seki
中科院分区：
文献类型：
--
作者：
T. Seki;Keigo Abe;Kiminobu Nakamura;Yuya Egawa;R. Miki;K. Juni;T. Seki
本文设计了一种由苯硼酸修饰的γ-环糊精（PBA-γ-CyD）和萘修饰的聚乙二醇（Naph-PEG）组成的分子项链--假聚轮烷（PPRX），用于开发糖响应性胰岛素给药系统。有趣的是，结构分析表明，通过我们的方法获得的Naph-PEG/PBA-γ-CyD PPRX是单链的，而使用亲本γ-CyD的普通PPRX是双链的。Naph-PEG/PBA-γ-CyD PPRX在pH 7.4时水溶性差;然而，糖的添加诱导PPRX的崩解，并且组分溶解，表明PBA部分充当糖传感器。我们还开发了一种由Naph-PEG-Ins和PBA-γ-CyD组成的PPRX，并证实了Naph-PEG-Ins的释放速率在添加糖后加快。
AbstractWe have designed a pseudopolyrotaxane (PPRX), known as a molecular necklace, consisting of phenylboronic acid-modified γ-cyclodextrin (PBA-γ-CyD) and naphthalene-modified polyethylene glycol (Naph-PEG) for developing sugar-responsive insulin delivery systems. Interestingly, structural analyses show that the Naph-PEG/PBA-γ-CyD PPRX obtained by our method was single stranded, whereas ordinary PPRXs using parent γ-CyD were double stranded. The Naph-PEG/PBA-γ-CyD PPRX was poorly water soluble at pH 7.4; however, sugar addition induced disintegration of the PPRX, and the components were dissolved, suggesting that the PBA moiety acts as a sugar sensor. We also have developed a PPRX consisting of Naph-PEG-appended insulin (Naph-PEG-Ins) and PBA-γ-CyD and have confirmed that the release rate of Naph-PEG-Ins was accelerated following sugar addition.Graphical abstract