Graphene Oxide-based Nanocomposite Enabled Highly Efficient Targeted Synergistic Therapy for Colorectal Cancer

Abstract Integrating different therapies into a single nanoplatform has shown great potential for synergistic anti-tumor therapy. In this work, we fabricated the graphene oxide (GO)-based nanosheets loaded with chemotherapeutic drug 5-fluorouracil (5-FU) and modified with GE11, which is an efficient ligand for epidermal growth factor receptor (EGFR). The nanocomposite system 5-FU/GO-PEG-GE11 was found to transfer 5-FU into EGFR-overexpressing HCT-116 cells effectively. The oxidation of glutathione in the tumor cells was found to be accelerated and then destroy the intracellular redox balance after irradiation. The 5-FU/GO-PEG-GE11 nanocomposites exhibited an enhanced synergistic anti-tumor efficacy both in vitro and in vivo. Tumor inhibition rate was 90% in subcutaneous colorectal cancer (CRC) bearing mouse model. The GO-based nanocomposites serve as a versatile platform integrated of PTT and chemotherapy with EGFR-targeting ability, which hold great promise for CRC treatment.