State Key Laboratory of Analytical Chemistry for Life Science and Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry and Chemical Engineering, Nanjing University , Nanjing, 210023, China.
Anal Chem. 2017 Oct 3;89(19):10239-10247. doi: 10.1021/acs.analchem.7b01582. Epub 2017 Sep 21.
It is a great challenge to design a drug delivery system with a controlled manner, especially one triggered by an exclusive endogenous disease marker and with an easily tracked release process. Herein, we developed a drug delivery platform of carbon dots which were connected to a stem-loop molecular beacon loaded with doxorubicin and polyethylene glycol modified folic acid. Such a platform enables one to release drugs on demand under the stimuli of endogenous microRNA-21, and turn on the fluorescence of carbon dots and doxorubicin, which allows one to monitor the drug release process. The intracellular experiment indicated that folic acid could mediate endocytosis of the nanocarrier, and the overexpressed endogenous microRNA-21 served as a unique key to unlock the drug nanocarrier by competitive hybridization with the molecular beacon, which finally resulted in fluorescence recovery and realized a chemotherapeutic effect within human breast cancer cells. The nanocarrier may have potential application in personalized treatment of different cancer subtypes in which the corresponding miRNAs are overexpressed.
设计一种可控的药物输送系统是一项巨大的挑战，特别是一种由独特的内源性疾病标志物触发、具有易于跟踪的释放过程的药物输送系统。在这里，我们开发了一种碳点药物输送平台，该平台连接到负载多柔比星和聚乙二醇修饰叶酸的茎环分子信标。这种平台能够在内源性 microRNA-21 的刺激下按需释放药物，并开启碳点和多柔比星的荧光，从而可以监测药物释放过程。细胞内实验表明，叶酸可以介导纳米载体的内吞作用，而过表达的内源性 microRNA-21 作为独特的钥匙，通过与分子信标竞争杂交来解锁药物纳米载体，最终导致荧光恢复，并在人乳腺癌细胞中实现化疗效果。该纳米载体可能在针对不同过表达相应 miRNAs 的癌症亚型的个性化治疗中有潜在应用。
