Zeng Qinghui, Shao Dan, He Xu, Ren Zhongyuan, Ji Wenyu, Shan Chongxin, Qu Songnan, Li Jing, Chen Li, Li Qin
State Key Laboratory of Luminescence and Applications, Changchun Institute of Optics, Fine Mechanics and Physics, Chinese Academy of Sciences, Dong_Nanhu Road 3888, Changchun 130033, China.
J Mater Chem B. 2016 Aug 14;4(30):5119-5126. doi: 10.1039/c6tb01259k. Epub 2016 Jul 8.
Fluorescent carbon dots (CDs) with a size smaller than 10 nm, excellent biocompatibility, and low to no cytotoxicity are considered as a rising star in nanomedicine. In this report, for the first time we demonstrate that green-emitting CDs with a carboxyl-rich surface can be employed as a trackable drug delivery agent for localized cancer treatment in a mouse model. The CDs are conjugated with the cancer drug, Doxorubicin (DOX), via non-covalent bonding, utilizing the native carboxyl groups on CDs and the amine moiety on DOX molecules. The pH difference between cancer and normal cells was successfully exploited as the triggering mechanism for DOX release. Our in vivo study demonstrated that the fluorescent CDs can serve as a targeted drug delivery system for localized therapy, and the stimuli-responsive non-covalent bonding between the nanodot carrier and the drug molecule is sufficiently stable in complex biological systems. Taken together, our work provides a strategy to promote the potential clinical application of CDs in cancer theranostics.
尺寸小于10纳米、具有出色生物相容性且细胞毒性低或无细胞毒性的荧光碳点（CDs）被视为纳米医学领域的一颗新星。在本报告中，我们首次证明，具有富含羧基表面的绿色发光CDs可作为一种可追踪的药物递送剂，用于小鼠模型中的局部癌症治疗。通过利用CDs上的天然羧基和阿霉素（DOX）分子上的胺部分，CDs通过非共价键与抗癌药物阿霉素（DOX）结合。成功利用癌细胞与正常细胞之间的pH差异作为DOX释放的触发机制。我们的体内研究表明，荧光CDs可作为局部治疗的靶向药物递送系统，并且纳米点载体与药物分子之间的刺激响应性非共价键在复杂的生物系统中足够稳定。综上所述，我们的工作提供了一种策略，以促进CDs在癌症诊疗中的潜在临床应用。
