Biomedical Applications of Aggregation‐Induced Emission‐Active BODIPY Dyes and Their Analogues

BODIPY dyes and their analogues have attracted considerable interest due to their structural diversity and functional versatility, holding significant importance in fields such as materials science, catalytic chemistry, and biomedicine. Studies have shown that the introduction of weakly covalent bonds and phenyl rotors into boron‐based scaffold can effectively twist the conjugated system, thereby imparting aggregation‐induced emission (AIE) characteristics. This strategy successfully addresses the issue of aggregation‐caused quenching commonly associated with the planar and rigid conjugated structures of conventional BODIPY dyes and their analogues. As a result, AIE‐active BODIPY dyes and their analogues exhibit higher sensitivity and superior fluorescence performance compared to traditional materials, broadening their applicability in bioimaging and phototherapeutic cancer treatment. This review summarizes recent advances in the biomedical applications of AIE‐active BODIPY dyes and their analogues, with a particular focus on organelle‐targeted imaging including lipid droplets, lysosomes, and mitochondria, as well as cancer phototherapies such as photodynamic and photothermal therapy (PDT and PTT). Finally, we discuss current challenges and limitations in the field and propose promising research directions to inspire future innovations for improving disease diagnosis and treatment efficacy, as well as for developing minimally invasive therapeutic strategies.