Huang Kaizong, Zhu Lingli, Wang Yunke, Mo Ran, Hua Zichun
The State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing, 210046, P. R. China.
J Mater Chem B. 2017 Aug 21;5(31):6356-6365. doi: 10.1039/c7tb00190h. Epub 2017 Jul 31.
Developing a smart cancer drug delivery carrier with enhanced cancer-targeting and effective drug release in tumors is critical for efficient cancer chemotherapy. Herein, we designed a pH-responsive copolymer (PEG-ELP[VH-70]) that entraps DOX into a hydrophobic core and self-assembles into smart DOX-loaded nanoparticles. The DOX-loaded nanoparticles were stabilized by Zn and disrupted as the pH drops from 7.4 to 5.6. An in vitro study demonstrated that the DOX-loaded nanoparticle system exhibited efficient internalization, triggered the release of DOX into the cytoplasm and enabled the inhibition of tumors effectively. When used to deliver chemotherapeutics to a murine cancer model, PEG-ELP[VH-70]/DOX accomplished a 4.8-fold suppressed effect relative to the free drug after intravenous injection. This simple strategy can promote preeminent stability for targeting hydrophobic drugs to tumor tissues.
开发一种具有增强的肿瘤靶向性和肿瘤内有效药物释放功能的智能癌症药物递送载体对于高效的癌症化疗至关重要。在此，我们设计了一种pH响应共聚物（PEG-ELP[VH-70]），它将阿霉素包裹在疏水核心中，并自组装成载有阿霉素的智能纳米颗粒。载有阿霉素的纳米颗粒通过锌稳定，并在pH从7.4降至5.6时解体。体外研究表明，载有阿霉素的纳米颗粒系统表现出高效内化，触发阿霉素释放到细胞质中，并有效抑制肿瘤。当用于将化疗药物递送至小鼠癌症模型时，PEG-ELP[VH-70]/阿霉素在静脉注射后相对于游离药物实现了4.8倍的抑制效果。这种简单的策略可以促进将疏水性药物靶向肿瘤组织的卓越稳定性。
