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Endogenous MicroRNA-Triggered and Real-Time Monitored Drug Release via Cascaded Energy Transfer Payloads
Analytical Chemistry ( IF 6.7 ) Pub Date : 2017-09-21 00:00:00 , DOI: 10.1021/acs.analchem.7b01582
Fan Yang 1 , Ting-Ting Zhang 1 , Shan-Shan Li 1 , Pei Song 1 , Kai Zhang 1 , Qi-Yuan Guan 1 , Bin Kang 1 , Jing-Juan Xu 1 , Hong-Yuan Chen 1
Affiliation  

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.

中文翻译:

通过级联的能量转移有效载荷触发的内源性MicroRNA触发和实时监控的药物释放

设计一种可控方式的药物输送系统是一个巨大的挑战,尤其是由专有的内源性疾病标记物触发并具有易于跟踪的释放过程的药物释放系统。本文中,我们开发了一个碳点药物递送平台,该碳点与装有阿霉素和聚乙二醇修饰叶酸的茎环分子信标相连。这种平台使人们能够在内源性microRNA-21的刺激下按需释放药物,并开启碳点和阿霉素的荧光,从而可以监测药物的释放过程。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是通过与分子信标竞争性杂交来解锁药物纳米载体的独特钥匙,最终导致荧光恢复,并在人乳腺癌细胞内实现了化学治疗作用。纳米载体可能在不同的癌症亚型的个性化治疗中具有潜在的应用,其中相应的miRNA过表达。
更新日期:2017-09-21
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