Multi‐functional Nanodrug Based on a Three‐dimensional Framework for Targeted Photo‐chemo Synergetic Cancer Therapy

Abstract Targeted synergistic therapy has broad prospects in tumor treatments. Here, a multi‐functional nanodrug GDYO‐CDDP/DOX@DSPE‐PEG‐MTX (GCDM) based on three traditional anticancer drugs (doxorubicin (DOX), cisplatin (CDDP) and methotrexate (MTX)) modified graphdiyne oxide (GDYO) is described, for diagnosis and targeted cancer photo‐chemo synergetic therapy. In this system, for the first time, these three traditional anti‐cancer drugs have played new roles and can reduce multidrug resistance through synergistic anti‐tumor effects. Cisplatin can be hybridized with GDYO to form a multifunctional and well‐dispersed three‐dimensional framework, which can not only be used as nano‐drug carriers to achieve high drug loading rates (40.3%), but also exhibit excellent photothermal conversion efficiency (47%) and good photodynamic effects under NIR irradiation. Doxorubicin (DOX) is loaded onto GDYO‐CDDP through π ‐ π stacking, which is used as an anticancer drug and as a fluorescent probe for nanodrug detection. Methotrexate (MTX) can be applied in tumor targeting and play a role in synergistic chemotherapy with DOX and CDDP. The synthesized multi‐functional nanodrug GCDM has good biocompatibility, active targeting, long‐term retention, sustained drug release, excellent fluorescence imaging capabilities, and remarkable photo‐chemo synergistic therapeutic effects.