Thiophene π-Bridge Manipulation of NIR-II AIEgens for Multimodal Tumor Phototheranostics

Angew Chem Int Ed Engl. 2024 Apr 2;63(14):e202318609. doi: 10.1002/anie.202318609. Epub 2024 Feb 29.

Abstract

The fabrication of a multimodal phototheranostic platform on the basis of single-component theranostic agent to afford both imaging and therapy simultaneously, is attractive yet full of challenges. The emergence of aggregation-induced emission luminogens (AIEgens), particularly those emit fluorescence in the second near-infrared window (NIR-II), provides a powerful tool for cancer treatment by virtue of adjustable pathway for radiative/non-radiative energy consumption, deeper penetration depth and aggregation-enhanced theranostic performance. Although bulky thiophene π-bridges such as ortho-alkylated thiophene, 3,4-ethoxylene dioxythiophene and benzo[c]thiophene are commonly adopted to construct NIR-II AIEgens, the subtle differentiation on their theranostic behaviours has yet to be comprehensively investigated. In this work, systematical investigations discovered that AIEgen BT-NS bearing benzo[c]thiophene possesses acceptable NIR-II fluorescence emission intensity, efficient reactive oxygen species generation, and high photothermal conversion efficiency. Eventually, by using of BT-NS nanoparticles, unprecedented performance on NIR-II fluorescence/photoacoustic/photothermal imaging-guided synergistic photodynamic/photothermal elimination of tumors was demonstrated. This study thus offers useful insights into developing versatile phototheranostic systems for clinical trials.

Keywords: NIR-II fluorescence imaging; aggregation-induced emission; multimodal phototheranostics; π-bridge engineering.

MeSH terms

  • Cell Line, Tumor
  • Humans
  • Nanoparticles* / therapeutic use
  • Neoplasms* / diagnostic imaging
  • Neoplasms* / therapy
  • Phototherapy / methods
  • Precision Medicine
  • Theranostic Nanomedicine / methods