State Key Laboratory of Analytical Chemistry for Life Science, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210093 (P.R. China).
Angew Chem Int Ed Engl. 2014 Feb 24;53(9):2371-5. doi: 10.1002/anie.201308920. Epub 2014 Jan 27.
The design of an ideal drug delivery system with targeted recognition and zero premature release, especially controlled and specific release that is triggered by an exclusive endogenous stimulus, is a great challenge. A traceable and aptamer-targeted drug nanocarrier has now been developed; the nanocarrier was obtained by capping mesoporous silica-coated quantum dots with a programmable DNA hybrid, and the drug release was controlled by microRNA. Once the nanocarriers had been delivered into HeLa cells by aptamer-mediated recognition and endocytosis, the overexpressed endogenous miR-21 served as an exclusive key to unlock the nanocarriers by competitive hybridization with the DNA hybrid, which led to a sustained lethality of the HeLa cells. If microRNA that is exclusively expressed in specific pathological cell was screened, a combination of chemotherapy and gene therapy should pave the way for a targeted and personalized treatment of human diseases.
设计一种理想的药物输送系统,具有靶向识别和零过早释放的功能,特别是在受到特定的内源性刺激时进行控制和特定的释放,这是一个巨大的挑战。现在已经开发出一种可追踪和适配体靶向的药物纳米载体;该纳米载体是通过用可编程 DNA 杂交体覆盖介孔硅涂层量子点而获得的,并且通过 microRNA 控制药物释放。一旦纳米载体通过适配体介导的识别和内吞作用被递送到 HeLa 细胞中,过表达的内源性 miR-21 就会作为一个专属的钥匙,通过与 DNA 杂交体进行竞争杂交来解锁纳米载体,从而导致 HeLa 细胞持续死亡。如果筛选出专门在特定病理细胞中表达的 microRNA,那么化疗和基因治疗的结合应该为针对人类疾病的靶向和个性化治疗铺平道路。