Zinc(II) Metalated Porphyrins as Photothermogenic Photosensitizers for Cancer Photodynamic/Photothermal Synergistic Therapy

Authors:
Publisher website
Google Scholar
Abstract
Porphyrin derivatives are the first-generation photosensitizers, and to design a strong NIR-absorbing porphyrin with good water solubility is highly desired for better therapeutic effect to treat tumors. Herein, three new porphyrin derivatives, 5,10,15,20-tetrakis(3,4- dimethoxyphenyl) porphyrin (P1), 5,10,15,20-tetrakis(3,4-dimethoxyphenyl) Zinc porphyrin (ZnP1), and 5,15-bis (3,4-dimethoxyphenyl)-10,20-bis ((4-methoxyphenyl)ethynyl) Zinc porphyrin (ZnP2) have been synthesized. Among them, ZnP2 shows the longest and most intensive Q-bands in the near-infrared (NIR) region, as endows it the strongest light-harvesting capability and deepest tumor tissue penetration. The three porphyrin derivatives were prepared into nanoparticles (NPs) via nanoprecipitation method, and the NPs exhibit good water dispersibility and passive tumor-targeting property through enhanced permeability and retention (EPR) effect. Furthermore, these NPs demonstrate both photodynamic and photothermal effects. Through systematical study of the singlet oxygen quantum yield and cytotoxicity of P1, ZnP1 and ZnP2 NPs in vitro on Hela cells, it is found that ZnP2 shows the highest singlet oxygen quantum yield (79%) and its NPs show the best therapeutic efficacy in vitro. In vivo experiments disclosed that ZnP2 NPs present high phototoxicity, low dark toxicity and excellent bio-compatibility, and could be used as a promising photothermogenic photosensitizer for cancer treatment.
Funding Information
  • Natural Science Foundation of Jiangsu Province (BK20161012)
  • National Natural Science Foundation of China (51273024, 61371066, 61525402, 61604071, 61775095)
  • Jiangsu Province (15KJA430006, 2015720, BE2017741)

This publication has 57 references indexed in Scilit: