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Macromol Biosci. 2015 Nov;15(11):1512-22. doi: 10.1002/mabi.201500156. Epub 2015 Jun 23.

Hydrolysis-Sensitive Dithiolethione Prodrug Micelles.

Author information

1
Frontier Research Base for Young Researchers and Department of Applied Chemistry, Graduate School of Engineering, Osaka University, 2-1 Yamadaoka, Suita, Osaka, 565-0871, Japan. urara.hasegawa@chem.eng.osaka-u.ac.jp.
2
Department of Applied Chemistry, Graduate School of Engineering, Osaka University, 2-1 Yamadaoka, Suita, Osaka, 565-0871, Japan.
3
Frontier Research Center and Department of Applied Chemistry, Graduate School of Engineering, Osaka University, 2-1 Yamadaoka, Suita, Osaka, 565-0871, Japan.

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.

KEYWORDS:

block copolymer; cytotoxicity; dithiolehthiones; micelle; prodrug

PMID:
26102371
DOI:
10.1002/mabi.201500156
[Indexed for MEDLINE]

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