The design and synthesis of water-soluble phototherapeutic agents with near-infrared (NIR) fluorescence emission is highly desirable for cancer diagnosis and treatment. Here, we report the construction of an amphiphilic perylene-derived photosensitizer, AP. AP shows NIR emission with large Stokes shift (130 nm) and high 1O2 quantum yield (22%). It can self-assemble into nanoparticles in aqueous solution with quenched fluorescence emission due to aggregation-induced quenching. Upon membrane anchoring, AP is able to disassemble into free monomer molecules and specifically "light up" the cell membrane without the usually required washing procedures. Furthermore, AP is subsequently used for the efficient photodynamic therapy against cancer cells and solid tumors. The in vitro and in vivo experiments clearly indicate that AP is suitable for biological imaging and can serve as a promising photosensitizer for tumor suppression.
Keywords: NIR fluorescence; controlled aggregation; perylene probe; phototherapy; wash-free imaging.