Development of a Water-Soluble BODIPY Photosensitizer for Photodynamic Therapy

In this study, we reported a photosensitizer design strategy that utilizes a lipophilic cation to enhance the cellular uptake of BODIPY photosensitizers. We designed and synthesized 8-Anisole-3,5-bis-(4-((12-(1-methyl-piperidinium iodide)dodecyl)oxy)phenyl)-4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (short as BO2), and investigated the solvent effect and singlet oxygen generation based on its absorption and emission spectra. Our experiments showed that BO2 maintains bright fluorescence, environmental insensitivity, photostability, and excellent singlet oxygen generation properties. In addition, cellular experiments demonstrated that BO2 exhibits good cellular uptake and photodamage. Therefore, we conclude that BO2 has potential applications in photodynamic therapy.