BODIPY-Based Photosensitizers in Photodynamic Therapy

Photodynamic therapy (PDT) harnesses light-activated molecules to generate cytotoxic reactive oxygen species for the selective ablation of pathological tissue. Among emerging photosensitisers, BODIPY (4,4-difluoro-4-bora-3a,4a-diaza-s-indacene) derivatives stand out for their intense absorption in the visible region, sharp emission profiles and remarkable photostability. Structural modifications—such as halogenation, heavy-atom incorporation and conjugation to targeting moieties—tailor intersystem crossing rates and singlet-oxygen yields, while appendages for water solubility and receptor recognition enhance cellular uptake and tissue specificity. Advances in nanoplatform integration and ligand-directed constructs have enabled simultaneous imaging and therapy, minimising off-target effects. Current research spans cancer, antimicrobial and immunomodulatory applications, reflecting the global ambition to deliver minimally invasive, image-guided phototherapies with improved safety and efficacy profiles.

Research from Nature Portfolio

Recent studies have produced water-soluble BODIPY nanoparticles functionalised with lactose ligands for liver-cancer targeting. These particles exhibit high fluorescence quantum yields and efficient singlet-oxygen generation under green light, enabling real-time imaging guidance and potent phototoxicity against hepatoma and cervical carcinoma cells. Foundational work on silylated, heavy-atom-containing BODIPY dyes covalently embedded in silica matrices demonstrated enhanced reactive oxygen species output alongside reduced dye leakage and preserved radiolabelling capability for PET imaging. In parallel, peptide-guided diiodo-BODIPY conjugates targeting the TrkC receptor have revealed an immunostimulatory dimension of PDT, promoting effector T-cell activation, suppressing regulatory T-cells, and achieving sustained tumour suppression both with and without light irradiation.

BODIPY-Based Photosensitizers in Photodynamic Therapy publication trend

The graph below shows the total number of articles in bodipy-based photosensitizers in photodynamic therapy across all publications each year (not limited to Nature Index journals).

Technical terms

Photodynamic therapy (PDT): A treatment modality in which light-activated photosensitisers produce cytotoxic oxygen species to destroy diseased cells.

BODIPY: A class of boron-dipyrromethene fluorophores valued for strong visible-light absorption, sharp emission and chemical tunability.

Singlet oxygen: An electronically excited form of molecular oxygen that induces oxidative damage to biomolecules.

Intersystem crossing (ISC): A non-radiative transition between singlet and triplet excited states that enables reactive oxygen species formation.

Heavy atom effect: The enhancement of intersystem crossing rates achieved by introducing heavy atoms (e.g. iodine, bromine) into a chromophore.

Quantum yield: The ratio of emitted photons or generated reactive species to absorbed photons, indicating photochemical efficiency.

References

1. Cationic BODIPY Photosensitizers for Mitochondrion-Targeted Fluorescence Cell-Imaging and Photodynamic Therapy. Pharmaceutics (2023).
2. Inherently Antimicrobial P(MMA-ran-DMAEMA) Copolymers Sensitive to Photodynamic Therapy: A Double Bactericidal Effect for Active Wound Dressing. International Journal of Molecular Sciences (2023).
3. BODIPY nanoparticles functionalized with lactose for cancer-targeted and fluorescence imaging-guided photodynamic therapy. Scientific Reports (2022).
4. BODIPY-doped silica nanoparticles with reduced dye leakage and enhanced singlet oxygen generation. Scientific Reports (2015).
5. Tropomyosin Receptor Kinase C Targeted Delivery of a Peptidomimetic Ligand-Photosensitizer Conjugate Induces Antitumor Immune Responses Following Photodynamic Therapy. Scientific Reports (2016).
6. BODIPYs in PDT: A Journey through the Most Interesting Molecules Produced in the Last 10 Years. International Journal of Molecular Sciences (2022).