Host−guest complexation-mediated codelivery of anticancer drug and photosensitizer for cancer photochemotherapy

Significance The combination of chemotherapy and photodynamic therapy opens up a promising way of overcoming drug resistance, incorporating different mechanisms of actions to achieve synergistic efficacy. However, the antitumor outcome of photodynamic therapy is greatly limited due to the unsatisfactory singlet oxygen generation caused by severe aggregation of the photosensitizer. To this end, we utilize a discrete metallacage containing therapeutic organoplatinum(II) to encapsulate a photosensitizer by forming an inclusion host–guest complex, facilitating the codelivery of chemotherapeutic agent and photosensitizer through nanoformulation. Benefiting from the enhanced permeability and retention effect and active targeting, the nanomedicine exhibits satisfactory antitumor performance against drug-resistant tumor. This pioneering work provides a distinct supramolecular methodology to prepare theranostic systems for multimodality imaging and therapy.