Evaluation of ketoprofen (R, S and RS) phototoxicity by a battery of in vitro assays

✍ Scribed by Francisco Boscá; Germano Carganico; JoséV. Castell; Maria J. Gómez-Lechón; Daniel Hernandez; David Mauleón; Luis A. Martínez; Miguel A. Miranda

• Publisher: Elsevier Science
• Year: 1995
• Tongue: English
• Weight: 524 KB
• Volume: 31
• Category: Article
• ISSN: 1011-1344
• DOI: 10.1016/1011-1344(95)07181-4

✦ Synopsis

The various enantiomers of ketoprofen (S and R) and its racemic form (R/S) exhibited comparable phototoxicities when examined by the following in vitro test systems: (a) effects of pre-irradiated drugs on cultured hepatocytes; (b) co-irradiation of the drugs with hepatocytes or fibroblasts; (c) photohaemolysis sensitized by the various ketoprofen stereoisomers; (d) dmg-photosensitized formation of iinoleic acid hydroperoxides. Inhibition of photohaemolysis and photodynamic lipid peroxidation by butylated hydroxyanisole and reduced glutathione .,.uggests that the phototoxicity of ketoprofen is associated with a radical chain (type I) peroxidation of membrane lipids, leading to cell lysis. In view of the above results it could be advantageous to use the pharmacologically active S( + ) enantiomer instead of the R/S form, since the lower doses required would result in a diminished phototoxic potential.