Reviewing the evolutive ACQ‐to‐AIE transformation of photosensitizers for phototheranostics

Abstract Photodynamic therapy (PDT) represents an emerging noninvasive treatment technique for cancers and various nonmalignant diseases, including infections. During the process of PDT, the physical and chemical properties of photosensitizers (PSs) critically determine the effectiveness of PDT. Traditional PSs have made great progress in clinical applications. One of the challenges is that traditional PSs suffer from aggregation‐caused quenching (ACQ) due to their discotic structures. Recently, aggregation‐induced emission PSs (AIE‐PSs) with a twisted propeller‐shaped conformation have been widely concerned because of high reactive oxygen species (ROS) generation efficiency, strong fluorescence efficiency, and resistance to photobleaching. However, AIE‐PSs also have some disadvantages, such as short absorption wavelengths and insufficient molar absorption coefficient. When the advantages and disadvantages of AIE‐PSs and ACQ‐PSs are complementary, combining ACQ‐PSs and AIE‐PSs is a “win‐to‐win” strategy. As far as we know, the conversion of traditional representative ACQ‐PSs to AIE‐PSs for phototheranostics has not been reviewed. In the review, we summarize the recent progress on the ACQ‐to‐AIE transformation of PSs and the strategies to achieve desirable theranostic applications. The review would be helpful to design more efficient ACQ‐AIE‐PSs in the future and to accelerate the development and clinical application of PDT.