Fluorescence imaging‐guided lipid droplets‐localized photodynamic therapy

Abstract Photodynamic therapy (PDT) has emerged as a promising strategy for cancer treatment due to its non‐invasive nature and high specificity toward malignant tissues. In recent years, a variety of protocols have been proposed to improve the PDT efficacy, of which organelle‐targeted PDT strategy is supposed to be quite promising. Particularly, lipid droplets (LDs)‐localized PDT attracts a lot of interest due to the inherent advantages such as abundant LDs in cancer cells and their close relation with ferroptosis. This review provides a comprehensive summary of the advancements of LDs‐localized photosensitizers (PSs) according to their chemical structures and functions. Especially, these PSs are featured with fluorescence emission, thereby facilitating an imaging‐guided phototherapy. The review highlights the cytocidal actions of these PSs, such as the cell death pathway and their cytotoxicity. Finally, some unresolved issues and challenges in this domain will be discussed.