Studies on the photostability and in vitro phototoxicity of Labetalol

Vincenza Andrisano, Roberto Ballardini, Patrizia Hrelia, Norma Cameli, Antonella Tosti, Roberto Gotti, Vanni Cavrini

Research output: Contribution to journalArticle

29 Scopus citations

Abstract

The purpose of this study was to obtain information on the photochemical and phototoxic properties of Labetalol, a beta-blocker drug. Preliminary information on the drug photoreactivity was achieved using a flow system with a photochemical reactor on-line with a diode array detection system. Photophysical and photochemical investigations on the drug were performed in aqueous solutions at different pH values using spectrophotometric and fluorimetric methods; the photodegradation quantum yield was found to be 2.7×10-3 at pH 5.8 and 1.5×10-2 at pH 11.5. Forced photodegradation of labetalol solutions under exposure to UVA-UVB radiations (xenon arc lamp) was monitored by reversed-phase liquid chromatography. The main photodegradation products were isolated and characterized by NMR and mass spectrometry; labetalol was found to give 3-amino-1-phenylbutane and salicylamide-4-carboxaldehyde as the main photoproducts. Preliminary phototoxic testings on human keratinocyte cultures were performed evaluating the viability of the cells by the neutral-red uptake assay; mutagenic and photomutagenicity tests were also carried out based on Salmonella typhimurium strains. As a result, labetalol was found to be photolabile,mainly in alkaline medium, but evidences of significant phototoxic and photomutagenic effects by the drug were not observed.

Original languageEnglish (US)
Pages (from-to)495-504
Number of pages10
JournalEuropean Journal of Pharmaceutical Sciences
Volume12
Issue number4
DOIs
StatePublished - Mar 6 2001
Externally publishedYes

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Keywords

  • Labetalol
  • Photomutagenicity
  • Photoproducts
  • Photostability
  • Phototoxicity
  • UVA-UVB radiation

ASJC Scopus subject areas

  • Pharmaceutical Science

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