2. Academic Validation
  3. Microenvironment-activatable nanoagent for real-time NIR-II monitoring and targeted therapy of arterial restenosis

Microenvironment-activatable nanoagent for real-time NIR-II monitoring and targeted therapy of arterial restenosis

  • Biomaterials. 2025 Jun 7:324:123482. doi: 10.1016/j.biomaterials.2025.123482.
Xianshe Meng 1,  Jianwen Song 2,  Huawen Meng 1,  Chenzhong Liao 1,  Zequn Yin 3,  Ke Gong 4,  Deling Kong 2,  Ji Qi 5,  Yajun Duan 6
Affiliations

Affiliations

  • 1 Key Laboratory of Metabolism and Regulation for Major Diseases of Anhui Higher Education Institutes, College of Food and Biological Engineering, Hefei University of Technology, Hefei, 230009, China.
  • 2 State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Bioactive Materials Ministry of Education, Frontiers Science Center for Cell Responses, and College of Life Sciences, Nankai University, Tianjin, 300071, China.
  • 3 Department of Cardiology, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, Anhui, 230001, China.
  • 4 Department of Physiology, Faculty of Basic Medical Sciences, Hubei Key Laboratory of Embryonic Stem Cell Research, Hubei University of Medicine, Shiyan, China.
  • 5 State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Bioactive Materials Ministry of Education, Frontiers Science Center for Cell Responses, and College of Life Sciences, Nankai University, Tianjin, 300071, China. Electronic address: qiji@nankai.edu.cn.
  • 6 Department of Cardiology, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, Anhui, 230001, China. Electronic address: yajunduan@ustc.edu.cn.
PMID: 40499225 DOI: 10.1016/j.biomaterials.2025.123482
Abstract

Arterial restenosis is a critical risk factor for life-threatening cardiovascular diseases. Precise intervention and real-time monitoring are extremely important but remain major clinical challenges. Here, we present an advanced theranostic nanoagent that integrates hypoxia-responsive second near-infrared (NIR-II) fluorescence imaging with hypoxia-activatable anti-proliferative therapy for real-time diagnostics and precision treatment. This nanoplatform is constructed by co-encapsulating a novel N-oxide-based molecular probe and a hypoxia-activatable prodrug tirapazamine (TPZ) into Osteopontin (OPN)-targeted liposomes. Under hypoxic conditions, the N-oxide probe undergoes conversion to its amine derivative, altering the intramolecular charge transfer properties and triggering turn-on NIR-II fluorescence signal. This property enables high-sensitivity, real-time monitoring of restenosis lesions in vivo. The nanoplatform exhibits dual hypoxia-responsive functionality: TPZ is selectively activated in hypoxic vascular lesions to inhibit vascular smooth muscle cell proliferation, and sustained OPN-mediated targeting promotes vascular repair. In guidewire-induced restenosis models, this system achieves simultaneous real-time monitoring of lesion progression via NIR-II imaging and significantly reduce restenosis while enhancing re-endothelialization. This study offers a promising strategy for developing high-performance theranostic nanoplatforms, enabling precise detection and improved treatment of restenosis-related diseases.

Keywords

Arterial restenosis; Dynamic monitoring; Hypoxia-activatable probe; Near-infrared II; Precise intervention.

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