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<p>Hypoxia is a significant feature in most of solid tumors. Hence, developing hypoxia-responsive phototheranostic system is still a challenge. In this contribution, a supramolecular assembly strategy based on sulfonate-functionalized azocalix[4]arene (SAC4A) and cationic aggregation-induced emission photosensitizer (namely TPA-H) was proposed for hypoxia-responsive bioimaging and photodynamic therapy (PDT). Upon supramolecular complexation of TPA-H and SAC4A through electrostatic interaction, the fluorescence and reactive oxygen species (ROS) generation of TPA-H were largely inhibited. In hypoxic tumors, the azo group of SAC4A can be reduced to aniline derivative and release the included TPA-H to recover its pristine fluorescence and ROS. Interestingly, the free TPA-H undergoes cell membrane-to-mitochondria translocation during cell imaging, achieving a real-time self-reporting PDT system. <i>In vivo</i> tumor imaging and therapy reveal that this as-prepared supramolecular complexes have good biosafety and efficient antitumor activity under hypoxia. Such hypoxia-responsive supramolecular photosensitizer system will enrich image-guided photodynamic therapy.</p>

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Self-reporting hypoxia-responsive supramolecular phototheranostic nanomaterials based on AIEgen and azocalixarene

  • 期刊论文

  • 发表日期：

    2025年1月2日

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  • Xiao-Wen Han,
  • Guo-Ling Zhang,
  • Pu Chen,
  • Jing Zhang,
  • Guogang Shan,
  • Chunxuan Qi,
  • Ben Zhong Tang,
  • Hai-Tao Feng

摘要

Hypoxia is a significant feature in most of solid tumors. Hence, developing hypoxia-responsive phototheranostic system is still a challenge. In this contribution, a supramolecular assembly strategy based on sulfonate-functionalized azocalix[4]arene (SAC4A) and cationic aggregation-induced emission photosensitizer (namely TPA-H) was proposed for hypoxia-responsive bioimaging and photodynamic therapy (PDT). Upon supramolecular complexation of TPA-H and SAC4A through electrostatic interaction, the fluorescence and reactive oxygen species (ROS) generation of TPA-H were largely inhibited. In hypoxic tumors, the azo group of SAC4A can be reduced to aniline derivative and release the included TPA-H to recover its pristine fluorescence and ROS. Interestingly, the free TPA-H undergoes cell membrane-to-mitochondria translocation during cell imaging, achieving a real-time self-reporting PDT system. In vivo tumor imaging and therapy reveal that this as-prepared supramolecular complexes have good biosafety and efficient antitumor activity under hypoxia. Such hypoxia-responsive supramolecular photosensitizer system will enrich image-guided photodynamic therapy.