The development of efficient organic sonosensitizers is crucial for sonodynamic
therapy (SDT) in the field of
cancer treatment. Herein, a new strategy for the development of efficient organic sonosensitizers based on triarylboron-doped acenethiophene scaffolds is presented. The attachment of
boron to the linear acenethiophenes lowers the lowest unoccupied molecular orbital (LUMO) energy, resulting in redshifted absorptions and emissions. After encapsulation with the amphiphilic
polymer DSPE-mPEG2000 , it is found that the nanostructured BAnTh-NPs and BTeTh-NPs (nanoparticles of BAnTh and BTeTh) shows efficient
hydroxyl radical (•
OH) generation under ultrasound (US) irradiation in aqueous
solution with almost no
phototoxicity, which can overcome the shortcomings of O2 -dependent SDT and avoid the potential cutaneous
phototoxicity issue. In vitro and in vivo therapeutic results validate that
boron-doped acenethiophenes as sonosensitizers enable high SDT efficiency with low
phototoxicity and good biocompatibility, indicating that
boron-functionalization of acenes is a promising strategy toward organic sonosensitizers for SDT.