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  3. A "simple" phototheranostic agent for high-performance type I photodynamic and photothermal synergistic cancer therapy

A "simple" phototheranostic agent for high-performance type I photodynamic and photothermal synergistic cancer therapy

  • J Colloid Interface Sci. 2025 Sep 25;703(Pt 1):139117. doi: 10.1016/j.jcis.2025.139117.
Xiang Liu 1,  Wenkai Zhang 2,  Wenzhao Shang 2,  Xianchao Du 3,  Hongjian Liu 4,  Ben Zhong Tang 5,  Dongfang Qiu 3,  Ruijin Yu 6,  Huifang Su 7
Affiliations

Affiliations

  • 1 College of Chemistry & Pharmacy, Northwest A&F University, Yangling, Shaanxi 712100, PR China; College of Chemistry and Pharmaceutical Engineering, Nanyang Normal University, Nanyang, Henan 473061, PR China.
  • 2 Department of Orthopaedic Surgery, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan 450052, PR China.
  • 3 College of Chemistry and Pharmaceutical Engineering, Nanyang Normal University, Nanyang, Henan 473061, PR China.
  • 4 Department of Orthopaedic Surgery, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan 450052, PR China. Electronic address: fccliuhj@zzu.edu.cn.
  • 5 School of Science and Engineering, Guangdong Basic Research Center of Excellence for Aggregate Science, Shenzhen Institute of Aggregate Science and Technology, The Chinese University of Hong Kong, Shenzhen (CUHK-Shenzhen), Guangdong 518172, PR China.. Electronic address: tangbenz@cuhk.edu.cn.
  • 6 College of Chemistry & Pharmacy, Northwest A&F University, Yangling, Shaanxi 712100, PR China. Electronic address: yuruijin@nwsuaf.edu.cn.
  • 7 Department of Orthopaedic Surgery, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan 450052, PR China. Electronic address: suhuif@alumni.sysu.edu.cn.
PMID: 41027051 DOI: 10.1016/j.jcis.2025.139117
Abstract

Synergistic type I photodynamic therapy (PDT) and photothermal therapy (PTT) offer a prospective approach to address the challenges posed by tumor hypoxia and heterogeneity, thereby achieving enhanced antitumor therapeutic outcomes. However, developing simple synthetic phototheranostic agents with efficient type I Reactive Oxygen Species (ROS) generation and effective photothermal conversion is still a significant task. In this study, fluorenone (FO), known for its potent electron-withdrawing properties, was conjugated with the rotor-type electron-donating triphenylamine (TPA) to construct a donor-acceptor-donor (D-A-D) structural aggregation-induced emission (AIE) Photosensitizer (TPAF), followed by the formation of nanoparticles (NPs) TPAF CNPs via self-assembly with DSPE-mPEG2000-cRGD and DSPE-mPEG2000. The TPAF CNPs effectively integrated efficient type I ROS with exceptional photothermal conversion capability. The fundamental photophysical and photochemical mechanisms underlying the synergistic effects of type I photodynamic and photothermal processes were explored through experimental and theoretical methods. In vitro and in vivo experiments showed that TPAF CNPs exhibited excellent photostability, good biocompatibility, enhanced tumor targeting, and outstanding synergistic type I PDT/PTT effects, achieving substantial antitumor therapeutic efficacy with a single injection and one laser irradiation. Overall, this study contributes to the growing field of high-performance type I PDT/PTT nanomedicine for synergistic phototheranostic applications.

Keywords

Fluorenone; Photothermal; Synergistic therapy; Type I photodynamic.

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