Polymeric Micelles with Water-Insoluble Drug as Hydrophobic Moiety for Drug Delivery
The hydrophobic block of polymeric micelles formed by amphiphilic copolymers has no direct therapeutical effect, and the metabolites of these hydrophobic segments might lead to some unexpected side effects. Here the hydrophobic core of polymeric micelles is replaced by highly water-insoluble drugs themselves, forming a new micellar drug delivery system. By grafting hydrophobic drugs of paclitaxel (PTX) onto the surface of hydrophilic hyperbranched poly(ether-ester) (HPEE), we constructed an amphiphilic copolymer (HPEE-PTX). HPEE-PTX could self-assemble into micellar nanoparticles in aqueous solution with tunable drug contents from 4.1 to 10.7％. Moreover, the hydrolysis of HPEE-PTX in serum resulted in the cumulative release of PTX. In vivo evaluation indicated that the dosage toleration of PTX in mice had been improved greatly and HPEE-PTX micellar nanoparticles could be used as an efficient prodrug with satisfactory therapeutical effect. We believe that most of the lipophilic drugs could improve their characters through this strategy.
Guolin Li Jinyao Liu Yan Pang Ruibin Wang Limin Mao Deyue Yan Xinyuan Zhu Jian Sun
School of Chemistry and Chemical Engineering Department of Oral and Maxillofacial Surgery, The First School of Chemistry and Chemical Engineering Instrumental Analysis Center, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong Un Department of Oral and Maxillofacial Surgery, The First Affiliated Hospital of Harbin Medical Univer School of Chemistry and Chemical Engineering Instrumental Analysis Center, State Key Laboratory of M Shanghai Key Laboratory of Stomatology, Department of Oral and Maxillofacial Surgery, The Ninth Peop
国际会议
上海
英文
39-49
2011-12-28（万方平台首次上网日期，不代表论文的发表时间）