An Asymmetrical Polymer Vesicle Strategy for Significantly Improving T1 MRI Sensitivity and Cancer-Targeted Drug Delivery

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• 作者：Qiuming Liu ; Shuai Chen ; Jing Chen ; Jianzhong Du
• 刊名：Macromolecules
• 出版年：2015
• 出版时间：February 10, 2015
• 年：2015
• 卷：48
• 期：3
• 页码：739-749
• 全文大小：637K
• ISSN：1520-5835

文摘

Traditional T₁ magnetic resonance imaging (MRI) contrast agents such as diethylenetriaminepentacetatic acid (DTPA) chelated gadolinium [Gd(III)] have poor sensitivity, leading to a risk of accumulated toxicity in vivo. To significantly improve the sensitivity of a T₁ MRI contrast agent and to enhance the efficacy of cancer chemotherapy, herein for the first time we report a noncytotoxic asymmetrical cancer targeting polymer vesicle based on R-poly(l-glutamic acid)-block-poly(蔚-caprolactone) [R is folic acid (FA) or DTPA]. Such asymmetrical vesicles have a cancer-targeting outer corona and a Gd(III)-chelating and drug-loading-enhancing inner corona, exhibiting an extremely high T₁ relaxivity (42.39 mM^鈥? s^鈥?, 8-fold better than DTPA-Gd) and anticancer drug loading efficiency (52.6% for doxorubicin hydrochloride, DOX路HCl). Moreover, the DOX-loaded vesicles exhibited excellent antitumor activity (2-fold better than free DOX). This 鈥渃helating-just-inside鈥?strategy for synthesizing asymmetrical polymer vesicles demonstrated promising potential theranostic applications in magnetic resonance imaging and cancer-targeted drug delivery.