Gong Peiwei, Du Jiuyao, Wang Dandan, Cao Bobo, Tian Meng, Wang Yuhua, Sun Lu, Ji Shuaijie, Liu Zhe
Institute of Anticancer Agents Development and Theranostic Application, The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine, Department of Chemistry and Chemical Engineering, Qufu Normal University, Qufu 273165, P. R. China.
J Mater Chem B. 2018 May 14;6(18):2769-2777. doi: 10.1039/c8tb00102b. Epub 2018 Apr 12.
The unique physicochemical properties and structure of fluorinated graphene (FG) hold great promise in biological fields, however, the strong hydrophobicity and chemical inertness heavily limit its further application, and the mechanism or utilization of FG as a drug nanocarrier has been rarely studied. Herein, a conceptual application of FG for loading doxorubicin (DOX) and cancer chemo-photothermal therapy is reported, and the interaction between FG and DOX was systematically investigated by density functional theory (DFT). To accomplish this, a mild method to synthesize stable and well-dispersed fluorinated graphene oxide (FGO) was developed, which exhibited excellent photothermal performance in the near infrared region (NIR), a high drug loading capacity (more than 200%), pH-triggered drug release, low cytotoxicity and good combination therapy effects. DFT results demonstrated that the introduction of fluorine provided more active sites for intermolecular interactions between DOX and FGO, and non-covalent interactions were the driving forces for drug loading and release. The presented method to employ FGO as an effective nanocarrier and the study of its interaction with drugs greatly broaden the further applications of FG, and provide new insights into developing novel drug delivery systems.
氟化石墨烯（FG）独特的物理化学性质和结构在生物领域具有巨大的应用前景，然而，其强疏水性和化学惰性严重限制了其进一步应用，并且FG作为药物纳米载体的作用机制或应用研究较少。在此，本文报道了FG用于负载阿霉素（DOX）及癌症化学-光热治疗的概念性应用，并通过密度泛函理论（DFT）系统研究了FG与DOX之间的相互作用。为此，开发了一种温和的方法来合成稳定且分散良好的氟化氧化石墨烯（FGO），其在近红外区域（NIR）表现出优异的光热性能、高载药能力（超过200%）、pH触发的药物释放、低细胞毒性以及良好的联合治疗效果。DFT结果表明，氟的引入为DOX与FGO之间的分子间相互作用提供了更多活性位点，非共价相互作用是药物负载和释放的驱动力。所提出的将FGO用作有效纳米载体的方法及其与药物相互作用的研究极大地拓宽了FG的进一步应用，并为开发新型药物递送系统提供了新的见解。
