Hydrolysis-Sensitive Dithiolethione Prodrug Micelles.

Urara Hasegawa, Naoya Tateishi, Hiroshi Uyama, André J van der Vlies

Index: Macromol. Biosci. 15 , 1512-22, (2015)

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Abstract

Prodrug micelles carrying 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione (ADT-OH), a compound possessing chemopreventive properties, are prepared from amphiphilic block copolymers linking ADT-OH via an ester bond using glycine (PAM-PGlyADT) and isoleucine linkers (PAM-PIleADT). The release of ADT-OH from the PAM-PIleADT micelles is much slower than the PAM-PGlyADT micelles. The PAM-PGlyADT micelles show comparable toxicity with ADT-OH in different cancer cell lines, whereas the PAM-PIleADT micelles are not toxic up to 400 µM. This ADT-ester prodrug micelle approach enables to modulate the release rate of ADT-OH and thus might find application in cancer therapy and prevention. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.