Supramolecular "all-in-one" nanodrug based on perylene diimide for dual-mode imaging guided PTT-chemotherapy.

The combination of photothermal therapy (PTT) and chemotherapy has been extensively investigated as a promising anticancer strategy, which can maximize therapeutic effects, reverse multidrug resistance, and reduce side effects. However, a conventional nanodrug delivery system incorporating a photothermal agent and chemotherapeutic drug together shows some disadvantages, including lower drug loading content, complex preparation process, and unpredictable safety risks of the carrier. Herein, a perylene diimide (PDI) derivative, PDI0, was synthesized as a photothermal agent, which could co-assemble with the chemotherapeutic drug DOX to develop novel multifunctional supramolecular nanodrugs. The prepared nanodrugs DP1, DP2, and DP3 with ultra-high drug loading capacity were carefully characterized by UV-vis absorption spectroscopy, fluorescence spectroscopy, DLS, and TEM. Notably, DP2 showed an appropriate average size of ∼73.4 nm. DP2 was sensitive to the stimuli of external light and internal lysosome acidic pH, and the photothermal conversion efficiency (η) was ∼54.34%. The photothermal and photoacoustic (PA) dual-mode imaging and anticancer effect were further evaluated by in vitro and in vivo investigations. Therefore, our prepared carrier-free nanodrug DP2 may have potential applications for dual-mode imaging guided synergistic PTT-chemotherapy. [ABSTRACT FROM AUTHOR]