作者
Marina Talelli, Maryam Iman, Amir K Varkouhi, Cristianne JF Rijcken, Raymond M Schiffelers, Tomas Etrych, Karel Ulbrich, Cornelus F van Nostrum, Twan Lammers, Gert Storm, Wim E Hennink
发表日期
2010/10/1
期刊
Biomaterials
卷号
31
期号
30
页码范围
7797-7804
出版商
Elsevier
简介
Doxorubicin (DOX) is clinically applied in cancer therapy, but its use is associated with dose limiting severe side effects. Core-crosslinked biodegradable polymeric micelles composed of poly(ethylene glycol)-b-poly[N-(2-hydroxypropyl) methacrylamide-lactate] (mPEG-b-p(HPMAm-Lacn)) diblock copolymers have shown prolonged circulation in the blood stream upon intravenous administration and enhanced tumor accumulation through the enhanced permeation and retention (EPR) effect. However a (physically) entrapped anticancer drug (paclitaxel) was previously shown to be rapidly eliminated from the circulation, likely because the drug was insufficiently retained in the micelles. To fully exploit the EPR effect for drug targeting, a DOX methacrylamide derivative (DOX-MA) was covalently incorporated into the micellar core by free radical polymerization. The structure of the doxorubicin derivative is susceptible to …
引用总数
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