Thiophene donor for NIR-II fluorescence imaging-guided photothermal/photodynamic/chemo combination therapy
Open accessAbstract
Organic fluorophores/photosensitizers have been widely used in biological imaging and photodynamic and photothermal combination therapy in the first near-infrared (NIR-I) window. However, their applications in the second near-infrared (NIR-II) window are still limited primarily due to low fluorescence quantum yields (QYs). Here, a boron dipyrromethene (BDP) is created as a molecularly engineered thiophene donor unit with high QYs to the redshift. Thiophene insertion initiates substantial redshifts of the absorbance as compared to its counterparts in which iodine is introduced. The fluorescent molecule can be triggered by an NIR laser with a single wavelength, thereby producing emission in the NIR-II windows. Single NIR laser-triggered phototherapeutic nanoparticles (NPs) are developed by encapsulating the BDP and the chemotherapeutic drug docetaxel (DTX) by using a synthetic amphiphilic poly(styrene-co-chloromethyl styrene)-graft-poly(ethylene glycol) functionalized with folic acid (FA). These BDP-T-N-DTX-FA NPs not only show superior solubility and high singlet oxygen QY (Φ Δ=62%) but also demonstrate single NIR laser-triggered multifunctional characteristics. After intravenous administration of the NPs into 4T1 tumor-bearing mice, the accumulation of the NPs in the tumor showed a high signal-to-background ratio (11.8). Furthermore, 4T1 tumors in mice were almost eradicated by DTX released from the BDP-T-N-DTX-FA NPs under single NIR laser excitation and the combination of photodynamic therapy (PDT) and photothermic therapy (PTT). STATEMENT OF SIGNIFICANCE: The application of organic photosensitizers is still limited primarily due to low fluorescence quantum yields (QYs) in the second near-infrared (NIR-II) window. Here, a boron dipyrromethene (BDP) as a molecularly engineered thiophene donor unit with high QYs to the redshift is created. Phototherapeutic nanoparticles (NPs) are developed by encapsulating the BDP and docetaxel (DTX) using a synthetic amphiphilic poly(styrene-co-chloromethyl styrene)-graft-poly(ethylene glycol) functionalized with folic acid (FA). These BDP-T-N-DTX-FA NPs not only show high singlet oxygen QY (Φ Δ=62%) but also demonstrate single NIR laser-triggered multifunctional characteristics and a high signal-to-background ratio (11.8). Furthermore, 4T1 tumors in mice were almost eradicated by DTX released from the BDP-T-N-DTX-FA NPs under single NIR laser excitation and the PDT/PTT combination therapy.
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BODIPY derivatives are an emerging class of small-molecule fluorophores that are key components in NIR dyes due to their strongly electron-withdrawing BF2 group and exceptional stability.
“BODIPY derivatives are an emerging class of small-molecule fluorophores that are key components in NIR dyes due to their strongly electron-withdrawing BF2 group and exceptional stability (Fig. 7 and Table 3)153–168.”
From Organic small-molecule NIR-II fluorophores for tumor phototheranostics (2026) · cites this paper as [155]
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- Authors
- Liu, Q., Tian, J., Tian, Y., Sun, Q., Sun, D., Liu, D., Wang, F., Xu, H., Ying, G., Wang, J., Yetisen, A. K., & Jiang, N.
- Affiliations
- China Academy of Chinese Medical Sciences (CN)
- China Pharmaceutical University (CN)
- Southern Medical University (CN)
- Chinese Academy of Sciences (CN)
- Nanjing Forestry University (CN)
- Stanford University (US)
- Brigham and Women's Hospital (US)
- Southern University of Science and Technology (CN)
- Imperial College London (GB)
- Harvard University (US)
- Corresponding author
- Xu, Haijun
- Ying, Guoliang
- Wang, Jigang
- Jiang, Nan
- ORCID
- Venue
- Acta Biomaterialia
- Publisher
- Elsevier BV
- Published
- 2021-06
- Volume
- 127
- Pages
- 287-297
- ISSN
- 1742-7061 (ISSN-L)
- OpenAlex
- W3149750019
- Cited by
- 43
- References
- 50
- Citations by year
- 2026: 6 · 2025: 9 · 2024: 11 · 2023: 8 · 2022: 9
- FWCI
- 2.12
- Type
- journal article
- Language
- en
- Update notices
- erratum (2022-04-01)
- Open access
- green
- doi.org
- Locations
- Acta Biomaterialia (publishedVersion)
- SSRN Electronic Journal (acceptedVersion)
- PubMed (publishedVersion)
- Funders
- Fundamental Research Funds for the Central Universities
- National Natural Science Foundation of China (21775166)
- Natural Science Foundation of Jiangsu Province (BK20151513, BK20180026)
- Topics
- Physical Sciences › Engineering › Biomedical Engineering › Nanoplatforms for cancer theranostics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Photodynamic Therapy Research Studies
- Physical Sciences › Materials Science › Materials Chemistry › Luminescence and Fluorescent Materials
- Keywords
- NIR-II fluorescence imaging, boron dipyrromethene, thiophene donor, photothermal therapy, photodynamic therapy, docetaxel, combination therapy, folic acid targeting, polymeric nanoparticles, tumor targeting, 4T1 breast cancer, near-infrared photosensitizer
- MeSH terms
- Animals, Photochemotherapy, Thiophenes, Photosensitizing Agents, Cell Line, Tumor, Mice, Nanoparticles, Optical Imaging
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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