Meso-tetraphenylporphyrin dimer derivative as a potential photosensitizer in photodynamic therapy.

Abstract

Studies on the synthesis, preliminary in vivo biological activity, singlet oxygen and fluorescence yields of a dimeric porphyrin (D1) are described. The pharmacokinetic behavior and photodynamic properties of the dimer D1 were examined in Balb/c mice bearing an MS-2 fibrosarcoma. Compound D1 shows a high selectivity for tumor localization (tumor/peritumoral tissue ratios of dye concentration ranging between ca 100 and 140 at 24 h after drug administration of 5.0-1.0 mg kg-1 into DL-alpha-dipalmitoylphosphatidylcholine liposomes). The phototherapeutic efficiency of dimer D1 was evaluated by following the growth curves of fibrosarcoma irradiated with red light (600-700 nm) with a total dose of 400 J cm-2, at 24 h after intravenous injection. Photodynamic therapy-treated tumors showed a significant delay in growth as compared to untreated control mice. The results obtained suggest that the porphyrin dimer D1 may be a promising candidate for further use in PDT experiments.

• Authors: M A Faustino, M G Neves, M G Vicente, J A Cavaleiro, M Neumann, H D Brauer, G Jori
• Journal: Photochemistry and photobiology (Photochem Photobiol) Vol. 66 Issue 4 Pg. 405-12 (Oct 1997) ISSN: 0031-8655 [Print] United States
• PMID: 9337611 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Photosensitizing Agents
• Porphyrins

Topics

• Animals
• Drug Design
• Female
• Fibrosarcoma (drug therapy)
• Mice
• Mice, Inbred BALB C
• Photochemistry
• Photochemotherapy (methods)
• Photosensitizing Agents (chemistry, pharmacokinetics, pharmacology)
• Porphyrins (chemistry, pharmacokinetics, pharmacology)