Self‐Assembly Induced Photosensitization of Long‐Tailed Heavy‐Atom‐Free BODIPY Derivatives for Photodynamic Therapy

Type I photosensitizers (PSs) are a promising approach for photodynamic therapy (PDT) since they can generate radicals that are tolerant to hypoxia. Thus, the development of highly efficient type I PSs is essential. Self-assembly is a promising strategy for developing novel PSs with desirable properties. Here, a simple and effective approach is developed to create heavy-atom-free PSs for PDT by self-assembling long-tailed boron dipyrromethene dyes (BODIPYs). The resulting aggregates BY-I16 and BY-I18 can efficiently convert their excited energy to the triplet state, producing reactive oxygen species that are essential for PDT. Furthermore, the aggregation and PDT performance can be regulated by adjusting the length of the tailed alkyl chains. As proof of concept, the efficacy of these heavy-atom-free PSs both in vitro and in vivo under both normoxic and hypoxic conditions is demonstrated.