Mitochondria-Targeting Organic Nanoparticles for Enhanced Photodynamic/Photothermal Therapy

Organelle-targeting techniques have been proved to be promising approaches for enhanced cancer treatment, especially phototherapy, because it can greatly improve the efficiency of photosensitizers. In this work, we designed and synthesized a mitochondria-targeting diketopyrrolopyrrole-based photosensitizer (DPP2+) for synergistic photodynamic/photothermal therapy upon irradiation. The obtained mitochondria-targeting nanoparticles (DPP2+ NPs) could produce thermal energy and singlet oxygen under 635 nm laser irradiation with ideal cytocompatibility. Importantly, DPP2+ NPs are more likely to enter the cells and target mitochondria. In in vitro and in vivo antitumor experiments, DPP2+ NPs showed highly effective antitumor effects, suggesting that mitochondria-targeting photosensitizers have potential for cancer treatment. The present work provides an alternative strategy to mitochondria-targeting molecular engineering and highlights the potential of organic nanomaterials in biomedical fields and cancer treatment.