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Exceptionally High Payload of the IR780 Iodide on Folic Acid-Functionalized Graphene Quantum Dots for Targeted Photothermal Therapy

Shuhua LiDepartment of Chemistry, Beijing Normal University, Beijing 100875, ChinaShixin ZhouDepartment of Cell Biology, School of Basic Medicine, Peking University Health Science Center, Beijing 100191, ChinaYunchao LiDepartment of Chemistry, Beijing Normal University, Beijing 100875, ChinaXiaohong LiDepartment of Chemistry, Beijing Normal University, Beijing 100875, ChinaJia ZhuDepartment of Chemistry, Beijing Normal University, Beijing 100875, ChinaLouzhen FanDepartment of Chemistry, Beijing Normal University, Beijing 100875, ChinaShihe YangDepartment of Chemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China
2017en
ABI

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The IR780 iodide (IR780) is recognized as an effective theranostic agent for simultaneous near-infrared fluorescence imaging and photothermal therapy (PTT). However, the rigid chloro-cyclohexenyl ring makes IR780 insoluble in almost all pharmaceutically acceptable solvents, which inevitably limits its clinical application. We report folic acid (FA)-functionalized graphene quantum dots (GQDs-FA) containing a large and intact sp2 domain with carboxyl groups around the edge. Such GQDs-FA possess exceptionally high loading capacity for IR780 via strong π–π stacking interactions, and the water solubility of IR780 is improved by over 2400-fold after loading onto GQDs-FA (IR780/GQDs-FA). IR780/GQDs-FA with an improved photostability, an enhanced tumor-targeting ability, and a high photothermal conversion efficiency of 87.9% were capable of producing sufficient hyperthermia to effectively kill cancer cells and completely eradicate tumors upon 808 nm laser irradiation. The present IR780/GQDs-FA may open up great opportunities for the effective PTT to treat cancer.

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