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The development of anticancer therapy is significant to human health but remains a huge challenge. Photodynamic therapy (PDT), inducing the synergistic mitochondrial dysfunction in cancer cells is a promising approach but suffer from the low efficiency in hypoxic microenvironment and deep‐seated tumors. Herein, to improve the outcomes of PDT for cancer treatment, a series of red fluorophores consisting of dual‐cationic triphenylphosphonium‐alkylated pyridinium and (substituted) triphenylamine are prepared as organelle‐targeting antitumor photosensitizers (PSs) with aggregation‐induced emission characteristics. These PSs can selectively accumulate at the mitochondria or lysosomes of cancer cells with both dark‐ and photo‐cytotoxicity, making them possess excellent killing effect on cancer cells and efficient inhibition of tumor growth in living mice. This study brings about new insight into the development of powerful cancer treatment. [ABSTRACT FROM AUTHOR]

A subcellular organelle-targeted delivery of anti-cancer drugs is a promising strategy to maximize the anti-cancer effects and minimize the adverse effects. Herein, we prepared a mitochondria-targeted drug delivery nanoplatform based on IR780 iodide (IR780) and titanium disulfide (TiS2) nanosheets. Due to the large specific surface area of TiS2 nanosheets, the nanoplatform could highly load anti-cancer drug resveratrol (RV). The as-prepared nanocomposite (IR780-TiS2/RV) was used for an efficacious photothermal-triggered tumor chemotherapy. IR780-TiS2/RV showed satisfactory stability and biocompatibility, and the loading ratio of RV and IR780 was about 112% and 56%, respectively. Upon the near-infrared (NIR) irradiation, the heat generated by IR780-TiS2/RV could trigger the RV release. Due to the conjugation with the mitochondria-specific IR780, IR780-TiS2/RV could target and accumulate in mitochondria and release RV when triggered by NIR to decrease the mitochondrial membrane potential, rapidly induce the upregulation of key intrinsic apoptotic factors such as cytochrome c, and initiate the caspase cascade, thereby achieving the chemotherapeutic effect. The IR780-TiS2/RV nanocomposite was demonstrated to have a high anti-tumor efficacy in vitro and in vivo as well as no remarkable tissue toxicity. We believe our study demonstrates that the NIR-triggered IR780-TiS2/RV nanoplatform could be a promising chemotherapeutic agent in clinical practice. [ABSTRACT FROM AUTHOR]