期刊
THERANOSTICS
卷 9, 期 6, 页码 1728-1740出版社
IVYSPRING INT PUBL
DOI: 10.7150/thno.30915
关键词
specific targeting peptide; MMP-2-controlled; shape transformation; dual-modal imaging; cancer therapy
资金
- National Natural Science Foundation of China [21775031, 81801766, 31870992]
- Beijing Natural Science Foundation [2172056, L172035]
- Youth Innovation Promotion CAS
- Key Research Program of the Chinese Academy of Sciences [KFZD-SW-210]
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.
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