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 Citations (Scopus)

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

Fingerprint

Labetalol
Phototoxic Dermatitis
Photolysis
Pharmaceutical Preparations
Neutral Red
Xenon
Reverse-Phase Chromatography
Salmonella typhimurium
Keratinocytes
Mass Spectrometry
Cell Survival
Radiation
In Vitro Techniques

Keywords

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

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Studies on the photostability and in vitro phototoxicity of Labetalol. / Andrisano, Vincenza; Ballardini, Roberto; Hrelia, Patrizia; Cameli, Norma; Tosti, Antonella; Gotti, Roberto; Cavrini, Vanni.

In: European Journal of Pharmaceutical Sciences, Vol. 12, No. 4, 06.03.2001, p. 495-504.

Research output: Contribution to journalArticle

Andrisano, V, Ballardini, R, Hrelia, P, Cameli, N, Tosti, A, Gotti, R & Cavrini, V 2001, 'Studies on the photostability and in vitro phototoxicity of Labetalol', European Journal of Pharmaceutical Sciences, vol. 12, no. 4, pp. 495-504. https://doi.org/10.1016/S0928-0987(00)00218-9
Andrisano, Vincenza ; Ballardini, Roberto ; Hrelia, Patrizia ; Cameli, Norma ; Tosti, Antonella ; Gotti, Roberto ; Cavrini, Vanni. / Studies on the photostability and in vitro phototoxicity of Labetalol. In: European Journal of Pharmaceutical Sciences. 2001 ; Vol. 12, No. 4. pp. 495-504.
@article{27a31b2ce6184312964e2af2e7899a13,
title = "Studies on the photostability and in vitro phototoxicity of Labetalol",
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.",
keywords = "Labetalol, Photomutagenicity, Photoproducts, Photostability, Phototoxicity, UVA-UVB radiation",
author = "Vincenza Andrisano and Roberto Ballardini and Patrizia Hrelia and Norma Cameli and Antonella Tosti and Roberto Gotti and Vanni Cavrini",
year = "2001",
month = "3",
day = "6",
doi = "10.1016/S0928-0987(00)00218-9",
language = "English",
volume = "12",
pages = "495--504",
journal = "European Journal of Pharmaceutical Sciences",
issn = "0928-0987",
publisher = "Elsevier",
number = "4",

}

TY - JOUR

T1 - Studies on the photostability and in vitro phototoxicity of Labetalol

AU - Andrisano, Vincenza

AU - Ballardini, Roberto

AU - Hrelia, Patrizia

AU - Cameli, Norma

AU - Tosti, Antonella

AU - Gotti, Roberto

AU - Cavrini, Vanni

PY - 2001/3/6

Y1 - 2001/3/6

N2 - 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.

AB - 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.

KW - Labetalol

KW - Photomutagenicity

KW - Photoproducts

KW - Photostability

KW - Phototoxicity

KW - UVA-UVB radiation

UR - http://www.scopus.com/inward/record.url?scp=0035110024&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0035110024&partnerID=8YFLogxK

U2 - 10.1016/S0928-0987(00)00218-9

DO - 10.1016/S0928-0987(00)00218-9

M3 - Article

C2 - 11231117

AN - SCOPUS:0035110024

VL - 12

SP - 495

EP - 504

JO - European Journal of Pharmaceutical Sciences

JF - European Journal of Pharmaceutical Sciences

SN - 0928-0987

IS - 4

ER -