Open AccessRationally Engineering Phototherapy Modules of Eosin-Conjugated Responsive Polymeric Nanocarriers via Intracellular Endocytic pH Gradients
Author(s) -
Guhuan Liu,
Jinming Hu,
Guoying Zhang,
Shiyong Liu
Publication year - 2015
Publication title -
bioconjugate chemistry
Language(s) - Uncategorized
Resource type - Journals
SCImago Journal Rank - 1.279
H-Index - 172
eISSN - 1520-4812
pISSN - 1043-1802
DOI - 10.1021/bc500548r
Subject(s) - chemistry , endocytic cycle , nanocarriers , micelle , photothermal therapy , intracellular , conjugated system , biophysics , photosensitizer , internalization , cytosol , protonation , photothermal effect , photochemistry , endosome , copolymer , photodynamic therapy , drug delivery , nanotechnology , endocytosis , organic chemistry , biochemistry , aqueous solution , polymer , ion , materials science , biology , cell , enzyme
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 (1)O2 generation capability, favoring a highly efficient photothermal module. Under mildly acidic pH associated with endolysosomes, protonation-triggered micelle-to-unimer transition results in recovered emission and enhanced photodynamic (1)O2 efficiency, which synergistically actuates release of encapsulated drugs, endosomal escape, and photochemical internalization processes.