Engineering of BODIPY-based theranostics for cancer therapy

Zhiqiang Mao, Ji Hyeon Kim, Jieun Lee, Hao Xiong, Fan Zhang, Jong Seung Kim

Research output: Contribution to journalReview articlepeer-review

40 Citations (Scopus)


In recent years, BODIPY-based theranostics have increasingly been used in cancer therapy and have achieved significant success. According to photochemical theories, the optical imaging (e.g., fluorescence [FLI]/photoacoustic [PAI]/photothermal imaging [PTI]) and phototherapy properties (photodynamic therapy [PDT] and photothermal therapy [PTT]) of BODIPY-based dyes can be well-tuned and balanced by chemical structural modifications. Furthermore, with the benefits of molecular/nanoparticle engineering, BODIPY-based theranostics can be endowed with versatile functionalities, including other cutting-edge therapeutic modalities, commendable tumor-targeting ability, and a delicate balance between imaging and therapy performance in a molecular/nano-entity, further enhancing its synergetic therapeutic potency and minimizing the undesirable side effects. In this review, we focus on BODIPY-based theranostics for tumor therapy and describe and discuss BODIPY-based FLI-guided chemotherapy, FLI-guided PDT, FLI-guided phototherapies, FLI-guided multi-modal therapies, and PAI-guided phototherapies, as well as multi-modal imaging-guided multi-modal therapies, particularly those that have become available in the last 3 years. The progress and bottlenecks of recent BODIPY-based theranostics are also itemized and discussed, describing the general design principles of BODIPY-based theranostics, with the aim of promoting the use of the theranostics in the clinical transformation of cancer therapy.

Original languageEnglish
Article number214908
JournalCoordination Chemistry Reviews
Publication statusPublished - 2023 Feb 1

Bibliographical note

Funding Information:
This work was financially supported by the National Natural Science Foundation of China (Nos. 22174034, 21904031), the Natural Science Foundation of Hubei Province (2021CFB305), and funded by the National Research Foundation of Korea (2018R1A3B1052702, 2019M3E5D1A01068998, 2019H1A2A1074096). Z. Mao thanks the China Scholarship Council (CSC, No. 202108420103).

Publisher Copyright:
© 2022 Elsevier B.V.


  • Cancer therapy
  • Photodynamic therapy
  • Photothermal therapy
  • Theranostic

ASJC Scopus subject areas

  • Materials Chemistry
  • General Chemistry
  • Inorganic Chemistry
  • Physical and Theoretical Chemistry


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