Spatiotemporal switching of respective phototherapy modes at the cellular level with minimum side eﬀects and high therapeutic eﬃcacy is a major challenge for cancer phototherapy. Herein we demonstrate how to address this issue by employing photosensitizer-conjugated pH-responsive block copolymers in combination with intracellular endocytic pH gradients. At neutral pH corresponding to extracellular and cytosol milieu, the copolymers self-assemble into micelles with prominently quenched fluorescence emission and low 1O2 generation capability, favouring highly efficient photothermal module. Under mildly acidic pH associated with endolysosomes, protonation-triggered micelle-to-unimer transition results in recovered emission and enhanced photodynamic 1O2 efficiency, which synergistically actuates release of encapsulated drugs, endosomal escape, and photochemical internalization processes.

Rationally engineering phototherapy modules of eosin-conjugated responsive polymeric nanocarriers via intracellular endocytic pH gradients

249th National Meeting (2015)

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