Activatable theranostic prodrug scaffold with tunable drug release rate for sequential photodynamic and chemotherapy

• DOI: 10.1002/smo.20230024
• Publication Date: 2024-02-20T16:53:12Z
• Authors: Si‐Yu Wang; Ying‐Hao Pan; Yu‐Chen Qu; Xiao‐Xiao Chen; Na Shao; Li‐Ya Niu; Qing‐Zheng Yang
• Keywords: BODIPY; Reactivity

Abstract Glutathione (GSH)‐activated prodrugs are promising for overcoming the limitations of conventional anti‐tumor drugs. However, current GSH‐responsive disulfide groups exhibit unregulated reactivity, making it impossible to precisely control drug release rate. We herein report a series with “three‐in‐one” molecular design by integrating fluorescence unit, stimuli‐responsive unit and chemodrug into one scaffold tunable aromatic nucleophilic substitution (S N Ar) reactivity. The rate these is tailored modification substituent different electron‐withdrawing or ‐donating abilities on BODIPY core. Furthermore, self‐assemble in water form nanoparticles that serve as photosensitizers produce reactive oxygen species upon irradiation photodynamic therapy (PDT). PDT process also increases concentration GSH cells, further promoting drugs chemotherapy. This strategy provides powerful platform sequential chemotherapy rates synergistic therapeutic effects.