Wang Xiaojuan, Sun Xing, Lao Jun, He Hua, Cheng Tiantian, Wang Mingqing, Wang Shengjie, Huang Fang
State Key Laboratory of Heavy Oil Processing and Center for Bioengineering and Biotechnology, China University of Petroleum (East China), 66 Changjiang West Road, Qingdao Economic Development Zone, Qingdao 266555, China.
State Key Laboratory of Heavy Oil Processing and Center for Bioengineering and Biotechnology, China University of Petroleum (East China), 66 Changjiang West Road, Qingdao Economic Development Zone, Qingdao 266555, China.
Colloids Surf B Biointerfaces. 2014 Oct 1;122:638-644. doi: 10.1016/j.colsurfb.2014.07.043. Epub 2014 Aug 7.
This study demonstrates that ligand-modified graphene quantum dots (GQDs) facilitate the simultaneous operation of multiple tasks without the need for external dyes. These tasks include selective cell labeling, targeted drug delivery, and real-time monitoring of cellular uptake. Folic acid (FA)-conjugated GQDs are synthesized and utilized to load the antitumor drug doxorubicin (DOX). The fabricated nanoassembly can unambiguously discriminate cancer cells from normal cells and efficiently deliver the drug to targeted cells. The inherent stable fluorescence of GQDs enables real-time monitoring of the cellular uptake of the DOX-GQD-FA nanoassembly and the consequent release of drugs. The nanoassembly is specifically internalized rapidly by HeLa cells via receptor-mediated endocytosis, whereas DOX release and accumulation are prolonged. In vitro toxicity data suggest that the DOX-GQD-FA nanoassembly can target HeLa cells differentially and efficiently while exhibiting significantly reduced cytotoxicity to non-target cells.
本研究表明，配体修饰的石墨烯量子点（GQDs）无需外部染料即可促进多项任务的同时操作。这些任务包括选择性细胞标记、靶向药物递送以及细胞摄取的实时监测。合成了叶酸（FA）共轭的GQDs并用于负载抗肿瘤药物阿霉素（DOX）。制备的纳米组装体能够明确区分癌细胞和正常细胞，并有效地将药物递送至靶向细胞。GQDs固有的稳定荧光能够实时监测DOX-GQD-FA纳米组装体的细胞摄取以及随后的药物释放。该纳米组装体通过受体介导的内吞作用被HeLa细胞快速特异性内化，而DOX的释放和积累则会延长。体外毒性数据表明，DOX-GQD-FA纳米组装体可以差异性地、有效地靶向HeLa细胞，同时对非靶向细胞的细胞毒性显著降低。
