An integrated targeting drug delivery system based on the hybridization of graphdiyne and MOFs for visualized cancer therapy.

Multimodal therapies have been regarded as promising strategies for cancer treatment as compared to conventional drug delivery systems that have various drawbacks in either low loading content, uncontrolled release, non-targeting or biotoxicity. We have developed a multifunctional three-dimensional tumor-targeting drug delivery system, Fe3O4@UIO-66-NH2/graphdiyne (FUGY), based on the hybridization of a novel two-dimensional material, graphdiyne (GDY), with a metal organic framework (MOFs) structure, Fe3O4@UIO-66-NH2 (FU). The FU MOF structure has superior ability for magnetic targeting, and was constructed by an in situ growth method in which it was surface-installed with GDY via amide bonds, as a carrier of anticancer drugs. The anticancer drug doxorubicin (DOX) was loaded onto FUGY and served as both an anticancer drug to treat the tumor and a fluorescence probe to ascertain the location of FUGY. The results show that FUGY exhibits a high drug loading content of 43.8% and an effective drug release around the tumor cells at pH 5.0. In particular, fluorescence imaging demonstrates that FUGY can deliver more anticancer drugs to tumor tissue than conventional drug delivery systems. Furthermore, FUGY exhibits superior therapeutic efficiencies with negligible side effects as compared to the direct administration of free DOX, both in vitro and in vivo. The obtained FUGY drug delivery system possesses ideal biocompatibility, sustained drug release, effective chemotherapeutic efficacy, and specific targeting abilities. Such a multimodal therapeutic system can facilitate new possibilities for multifunctional drug delivery systems.