Journal Article Sugar-responsive pseudopolyrotaxanes and their application in sugar-induced release of PEGylated insulin

関, 智宏  ,  阿部, 圭吾  ,  中村, 公薫  ,  江川, 祐哉  ,  三木, 涼太郎  ,  從二, 和彦  ,  関, 俊暢

82 ( 3-4 )  , pp.417 - 424 , 2015-03-26 , Springer
We 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.

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