Title of Paper:Poly(photosensitizer) Nanoparticles for Enhanced in Vivo Photodynamic Therapy by Interrupting the pi-pi Stacking and Extending Circulation Time

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Date of Publication:2019-05-22

Journal:ACS APPLIED MATERIALS & INTERFACES

Included Journals:PubMed、SCIE、EI

Volume:11

Issue:20

Page Number:18224-18232

ISSN No.:1944-8244

Key Words:photodynamic therapy; pi-pi interactions; ROS degradable poly(TPP); quantitative TPP loading; improved singlet oxygen quantum yield

Abstract:The natural planar and rigid structures of most of the hydrophobic photosensitizers (PSs) [such as tetraphenyl porphyrin (TPP)] significantly reduce their loading efficiencies in polymeric nanoparticles (NPs) because of the strong pi-pi interaction-induced aggregation. This aggregation-caused quenching will further reduce the quantum yield of singlet oxygen (O-1(2)) generation and weaken the efficiency of photodynamic therapy (PDT). In addition, the small molecular PSs exhibit short tumor retention time and tend to be easily cleared once released. Herein, poly(TPP) NPs, prepared by cross-linking of reactive oxygen species degradable, thioketal linkers and TPP derivatives, followed by coprecipitation, were first developed with quantitative loading efficiency (>99%), uniform NP sizes (without aggregation), increased singlet oxygen quantum yield (Phi(Delta) = 0.79 in dimethyl sulfoxide compared with 0.52 for original TPP), increased in vitro phototoxicity, extended tumor retention time, light-triggered on-demand release, and enhanced in vivo antitumor efficacy, which comprehensively address the multiple issues for most of the PSs in the PDT area.