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Severe aggregation-caused quenching and the lack of special organelle targeting in conventional photosensitizers (PSs) have limited their advantages in terms of their accurate spatial–temporal control and noninvasive features. Furthermore, severe tumor hypoxia equally diminished the effectiveness of treatment. Herein, a series of aggregation-induced emission (AIE) PSs with precise targeting of organelles are synthesized by simply regulating the molecular structure. The rotation of the donor in the molecule was optimized by altering the tail chain of the triphenylamine derivative, which inhibited nonradiative internal conversion and promoted intersystem crossing to facilitate the free radical generation, and the production efficiency of the type I reactive oxygen species exceeds that of the commercial indicator rose bengal (3-fold). The optimal AIE PS named BETTP can specifically target mitochondria and recognize cancer cells. Simultaneously, live/dead cell costaining assays and flow cytometry validated that BETTP nanoparticles (NPs) have the ability to efficaciously ablate cancer cells in hypoxic conditions after encapsulating BETTP into carriers as nanoparticles. In addition, BETTP NPs also manifest superior performance during near-infrared imaging-guided type I photodynamic therapy in solid tumors. Such BETTP NPs demonstrate the critical feasibility of achieving precise delivery of drugs and targeting of organelles for precise therapy in hypoxic environments, providing a reliable reference for tumor hypoxia challenges. [ABSTRACT FROM AUTHOR]

Design and synthesis of water-soluble near-infrared (NIR) emissive fluorescent molecules with aggregation-induced emission (AIE) characteristics, perfect signal-to-noise ratio for imaging of organelle, and photodynamic therapy (PDT) functions has received enormous attention. However, the dual-functional NIR AIEgens of high-fidelity tracking lysosome and ablation cancer cells was rarely reported. Herein, a series of AIE luminogens (AIEgens) with a typical AIE effect, good biocompatibility, superior photostability, high brightness, and excellent reactive oxygen species (ROS) generation ability were developed, which had different electronic push-pull strength and conjugate system size in the molecular structure. These AIEgens could specifically "light up" and dynamically long-term track the lysosomes in living cells and zebrafish with ultrahigh colocalization imaging Pearson's correlation coefficients (Rr: 0.9687) and overlap coefficient ( R : 0.9967). Additionally, the MPAT of NIR luminescence as a photosensitizer was used for photodynamic ablation of cancer cells, owing to prompt generation of the ROS under green light irradiation (495-530 nm, 10 mW cm -2 ). Hence, this research not only expands the application range of NIR AIEgens but also provides useful insights into design of split-new method for the treatment of cancer.