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MMP-2-Controlled Transforming Micelles for Heterogeneic Targeting and Programmable Cancer Therapy
时间:2019-08-14 11:38:18
分类:Theranostics
作品信息

期刊

Theranostics

标题

MMP-2-Controlled Transforming Micelles for Heterogeneic Targeting and Programmable Cancer Therapy

作者

Zihua Wang, Yuehua Wang, Xiangqian Jia, Qiuju Han, Yixia Qian, Qian Li, Junfeng Xiang, Qian Wang, Zhiyuan Hu, Weizhi Wang

摘要

Herein, through the active-peptide-functionalization, we developed a nanoscale micelles system (named HEKM) which consists of tumor microenvironment-regulated shape-changing with specific recognition abilities for enhanced cellular targeting, internalization and therapy of heterogeneic tumors. As a result, HEKMs could recognize and bind the tumor heterogeneity marker EGFR-HER2 complex, which led to an enhanced tumor targeting effect. In particular, HEKMs could self-assemble into nanorods under normal physiological conditions while transform into nanospheres in the tumor extracellular microenvironment by a sensitive response to matrix metalloproteinase-2 (MMP-2). The nanorods could prolong the blood circulation time while the nanospheres could accelerate tissue penetration in tumors. In vivo dual-modal targeted imaging was realized by FRET-fluorophore conjugation and gadolinium loading in HEKMs. Tumor cell apoptosis was achieved by proapoptotic element integration. The in vitro and in vivo studies both demonstrated that these rationally designed, shape-changing and targeting micelles could achieve maximized drug efficacy and minimum side effects.

原文链接

http://http://www.thno.org/v09p1728

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