Photodynamic Therapy with Porphyrin-Based Photosensitizers

Photodynamic therapy (PDT) utilises the convergence of light, oxygen and a photosensitizing agent to elicit selective cytotoxicity in target tissues. Porphyrin-based photosensitizers, owing to their strong absorption in the visible to near-infrared region, predictable photophysical properties and propensity for chemical modification, have emerged as leading compounds in this field. Upon illumination, these macrocycles transfer energy to molecular oxygen to yield reactive oxygen species—most notably singlet oxygen—that induce cell death via necrosis, apoptosis or autophagy. Advances in porphyrin chemistry have yielded second- and third-generation agents featuring targeted delivery motifs, enhanced tissue penetration and reduced off-target phototoxicity. Clinically, porphyrin-derived agents have found application in oncology, dermatology and antimicrobial therapies, with ongoing efforts to refine their pharmacokinetics and to integrate PDT with immunotherapy and image-guided modalities.

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Photodynamic Therapy with Porphyrin-Based Photosensitizers publication trend

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

Technical terms

Photosensitiser: A molecule that, upon absorption of light, transfers energy to oxygen or other substrates to generate cytotoxic species.

Porphyrin: A cyclic tetrapyrrole macrocycle that forms the core of many natural and synthetic photosensitizers.

Singlet oxygen: An electronically excited form of molecular oxygen responsible for the majority of PDT-induced cellular damage.

Reactive oxygen species: Chemically reactive derivatives of oxygen, including singlet oxygen, superoxide and peroxide, that mediate phototoxic effects.

Phototoxicity: Damage to cells or tissues resulting from light-activated photosensitizers.

Chlorin: A hydrogenated derivative of porphyrin with a red-shifted absorption spectrum, allowing deeper tissue penetration.

Glycoporphyrin: A porphyrin conjugated to carbohydrate moieties to enhance water solubility and selective uptake by target cells.

References

1. Porphyrin photosensitizers in photodynamic therapy and its applications. Oncotarget (2017).
2. Chemical approaches for the enhancement of porphyrin skeleton-based photodynamic therapy. Journal of Enzyme Inhibition and Medicinal Chemistry (2020).
3. Sonogashira cross-coupling as a key step in the synthesis of new glycoporphyrins. Organic Chemistry Frontiers (2022).
4. A Basic Study of Photodynamic Therapy with Glucose-Conjugated Chlorin e6 Using Mammary Carcinoma Xenografts. Cancers (2019).
5. Potential of Photodynamic Therapy Based on Sugar-Conjugated Photosensitizers. Journal of Clinical Medicine (2021).
6. A next-generation bifunctional photosensitizer with improved water-solubility for photodynamic therapy and diagnosis. Oncotarget (2016).