Key Laboratory of Biomedical Polymers of Ministry of Education & Department of Chemistry, Wuhan University, Wuhan 430072, PR China.
Biomaterials. 2013 Nov;34(34):8798-807. doi: 10.1016/j.biomaterials.2013.07.084. Epub 2013 Aug 9.
A novel strategy to construct a therapeutic system based on functionalized AuNPs which can specifically respond to tumor microenvironment was reported. In the therapeutic system, doxorubicin was conjugated to AuNPs via thiol-Au bond by using a peptide substrate, CPLGLAGG, which can be specifically cleaved by the protease. In vivo study shows that after injection of the functionalized AuNPs to the tumor-bearing mice, the over-expressed protease of MMP-2 in tumor tissue and intracellular GSH can lead to the rapid release of the anti-tumor drug (doxorubicin) from the functionalized AuNPs to inhibit tumor growth and realize fluorescently imaging simultaneously. The functionalized AuNPs with tumor-triggered drug release property can further improve the efficacy and reduce side effects significantly.
一种新策略构建了基于功能化金纳米粒子的治疗体系，该体系可以特异性响应肿瘤微环境。在治疗体系中，阿霉素通过巯基-金键与 AuNPs 相连，使用的是一种可以被蛋白酶特异性切割的肽底物 CPLGLAGG。体内研究表明，将功能化的 AuNPs 注射到荷瘤小鼠后，肿瘤组织中 MMP-2 过表达的蛋白酶和细胞内 GSH 可以导致阿霉素从功能化 AuNPs 中快速释放，从而抑制肿瘤生长并同时实现荧光成像。具有肿瘤触发药物释放特性的功能化 AuNPs 可以进一步显著提高疗效并降低副作用。
