Micellization of antineoplastic agent to significantly upregulate efficacy and security
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Updated: Apr 21, 2026

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Chen Li1, Weiguo Xu, Jianxun Ding
1Department of Orthopedics, The Second Hospital of Jilin University, Changchun, 130041, P. R. China.
Abstract:
The amphiphilic diblock copolymer composed of methoxy poly(ethylene glycol) and racemic oligoleucine was synthesized which formed into micelle with uniform size in aqueous environment. Doxorubicin (DOX) was loaded into micelle aided by noncovalent interactions with high drug loading efficiency. The DOX-loaded micelle (referred as M-DOX) demonstrated the sustained drug release in vitro and excellent antiproliferative capability toward both MG63 and Saos-2 cells. Furthermore, for both MG63 and Saos-2-xenografted BALB/c nude mouse models, M-DOX exhibited enhanced intratumoral distribution, improved antitumor efficacy, and reduced side effects compared with free DOX. Therefore, the polypeptide micelle showed a bright prospect for controlled delivery of antitumor drugs in vivo.
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