8-Hydroxyquinoline functionalized covalent organic framework as a pH sensitive carrier for drug delivery

• Published in: Materials Science & Engineering C Vol. 117; p. 111243
• Main Authors: Jia, Yutao, Zhang, Lina, He, Binnan, Lin, Yulong, Wang, Jing, Li, Meng
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.12.2020; Elsevier BV
• Subjects: 5-Fluorouracil; 8-Hydroxyquinoline; Anticancer properties; Biocompatibility; Cancer; Cell culture; Controlled release; Crystal structure; Drug delivery; Drug Delivery Systems; Hydrogen-Ion Concentration; Hydroxyquinoline; Materials science; Metal-Organic Frameworks; Nitrogen atoms; Organic covalent framework; Oxyquinoline; pH effects; pH sensitive; Pharmaceutical Preparations; Pore size; Porosity; Quinoline; Sensitivity; Organic covalent framework; 8-Hydroxyquinoline; pH sensitive; Drug delivery; 5-Fluorouracil
• ISSN: 0928-4931; 1873-0191
• DOI: 10.1016/j.msec.2020.111243

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 5-FU@COF-HQ) 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, 5-FU@COF-HQ-treated B16F10 cell-induced tumor models showed that 5-FU@COF-HQ 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. [Display omitted] •8-Hydroxyquinoline functionalized COF (COF-HQ) was used as drug carrier.•The introduction of quinoline group effectively improved the drug loading capacity.•COF-HQ showed good dispersion, stability and biocompatibility.•COF-HQ exhibited a pH-dependent drug release behavior.•5-Fluorouracil loaded COF-HQ showed excellent tumor suppressing ability in vivo.