Supramolecular chemistry provides a “bottom-up” method to fabricate nanostructures for biomedical applications. Hence, we report a facile strategy to directly assemble a phthalocyanine photosensitizer (PcS) with an anticancer drug mitoxantrone (MA) to form uniform nanostructures (PcS-MA), which not only display nanoscale optical properties but also have the capability of undergoing nucleic acid-responsive disassembly.

The effort focused on the design of a stimuli-responsive supramolecular nanostructure, composing a PS and an anticancer agent. This coassembly was also designed to display nanoscale optical properties as well as activatable singlet oxygen (¹O₂) generation and chemotherapeutic abilities.

In vivo evaluations demonstrate that PcS-MA nanostructures have a high level of accumulation in tumor tissues, are capable of being used for cancer imaging, and have significantly improved anticancer effect compared to that of PcS. This study indicates a novel strategy for overcoming the limitations of photodynamic cancer therapy.