Micellization of antineoplastic agent to significantly upregulate efficacy and security.
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.
Department of Orthopedics, The Second Hospital of Jilin University, Changchun, 130041, P. R. China.
Chen
C
Li
Weiguo
W
Xu
Jianxun
J
Ding
Ying
Y
Zhang
Jincheng
J
Wang
Xiuli
X
Zhuang
Xuesi
X
Chen
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001835:Body Weight / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004317:Doxorubicin / Q000494:pharmacology; D000067493:Dynamic Light Scattering; D005260:Female; D005434:Flow Cytometry; D005453:Fluorescence; D006801:Humans; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D008823:Micelles; D011092:Polyethylene Glycols / Q000737:chemistry; D066244:Proton Magnetic Resonance Spectroscopy; D017550:Spectroscopy, Fourier Transform Infrared; D016896:Treatment Outcome; D015854:Up-Regulation / Q000187:drug effects*; D014781:Viscera / Q000187:drug effects / Q000473:pathology
D000970:Antineoplastic Agents; D008823:Micelles; D011092:Polyethylene Glycols; D004317:Doxorubicin; C028210:monomethoxypolyethylene glycol
chemotherapy; diblock copolymers; drug delivery systems; nanotechnology; noncovalent interaction