A porous 8-hydroxyquinoline functionalized organic covalent framework (named COF-HQ) was synthesized. The as-prepared COF-HQ showed stable crystal structure, suitable pore size, excellent dispersibility in physiological solution and pH sensitivity, which would be employed as a potential nanocarrier for drug transport and controlled release. The drug loading experiment with 5-Fluorouracil (5-FU) as the model molecule proved that the drug loading capacity of COF-HQ was significantly improved due to the introduction of quinoline groups. The drug release profiles of 5-FU from 5-FU loaded COF-HQ (termed [email protected]) under different pH showed that its release was controlled by pH owing to the pH sensitivity of conjugated nitrogen atoms from quinoline groups and CN. The in vitro hemolysis and in vivo biocompatibility experiments further verified the good biocompatibility of COF-HQ. Importantly, [email protected] B16F10 cell-induced tumor models showed that [email protected] displayed enhanced anti-tumor efficacy than other groups. These results suggested that the drug-loading COF-HQ delivery system showed the potential for effective cancer therapy with advantages of high drug loading, good biocompatibility and the pH-sensitive release of the tumor microenvironment. Overall, our research provided a new functionalized COF-HQ drug delivery system, which further expanded the application of COFs as carriers in the field of cancer treatment.

合成了多孔的8-羟基喹啉官能化的有机共价骨架（命名为COF-HQ）。所制备的COF-HQ具有稳定的晶体结构，合适的孔径，在生理溶液中的优异分散性和pH敏感性，可作为潜在的纳米载体进行药物转运和控释。以5-氟尿嘧啶（5-FU）为模型分子的载药实验证明，由于引入了喹啉基，COF-HQ的载药量得到了显着提高。5-FU在不同pH下从装有5-FU的COF-HQ（称为[电子邮件保护]）的药物释放曲线表明，由于喹啉基和C N共轭氮原子的pH敏感性，其释放受pH控制。在体外溶血和体内生物相容性实验进一步验证了COF-HQ的良好生物相容性。重要的是，[电子邮件保护的] B16F10细胞诱导的肿瘤模型显示[电子邮件保护的]显示出比其他组更高的抗肿瘤功效。这些结果表明，载药COF-HQ递送系统显示出有效的癌症治疗潜能，具有载药量高，生物相容性好以及肿瘤微环境对pH敏感的释放等优点。总体而言，我们的研究提供了一种新的功能化COF-HQ药物递送系统，进一步扩展了COF作为载体在癌症治疗领域中的应用。