Amphiphilic Fullerene‐BODIPY Photosensitizers for Targeted Photodynamic Therapy

Nanotheranostic tailor‐made carriers are potent platforms for the treatment of cancer that propound a number of advantages over conventional agents for photodynamic therapy (PDT). Herein, four new heavy atom free amphiphilic glucose‐BODIPY‐fullerene dyads (14–17) endowed with carbohydrate units in the styryl units, which can also form nanomicelles (14–17NM) with Tween 80 for PDT are reported. Glucose‐BODIPY‐fullerene systems (14–17) and related nanomicelles (14‐17NM) have been prepared to emcee efficient singlet oxygen generation upon light irradiation. In vitro anti‐tumor effects of the compounds 14–17 and 14–17NM in the presence of light and in darkness have been investigated with K562 human chronic myelogenous leukemia suspension cells. Anti‐tumor toxicity upon light irradiation was due to the formation of singlet oxygen and reactive oxygen species (ROS). This study may provide an accomplished example of efficient PDT applications based on nanovehicles fabricated with universal spin converter, fullerene, light harvesting unit, BODIPY dyes conjugated with targeting units to fight against cancer. Targeted photosensitizers are crucial for cancer treatment. In this study, amphiphilic BODIPY‐fullerene nanocarriers bearing glucose units and their nanomicelles were prepared. Results of in vitro photodynamic therapy (PDT) studies indicate that these platforms are highly effective against tumor cells. This approach may expand the applications of fullerene‐mediated PDT.