▎ 摘　　要

Multimodal and synergistic therapy of cancer has appeared as one of the most promising strategies in treating cancer. Here, we report a supramolecular hierarchical nanocomposite for combination photodynamic, photothermal, and chemotherapy. Graphene oxide (GO, photothermal agent for photothermal therapy, PTT), protoporphyrin IX (PpIX, photosensitizer for photodynamic therapy, PDT), and hydrophilic anticancer drug doxorubicin hydrochloride (DOXHCl, therapeutic for chemotherapy) are involved in hierarchical self-assembled nanocomposites via supramolecular interactions. PEGylated PpIX (PEG-PpIX) is prepared to improve the stability of GO in physiological conditions. The nanocomposite GO(PEG-PpIX) is non-cytotoxic in the dark and phototoxic with light irradiation to exhibit efficient PTT and PDT effects. The drug loading content of the nanocomposite DOX/GO(PEG-PpIX) is as high as 15.9% and the drug release shows a pH-dependent profile. The combined PDT, PTT, and chemotherapy shows an excellent in vivo antitumor effect and side effect reduction. This work presents a facile yet robust strategy to fabricate a nanocomposite for multimodal synergistic therapy.