fr
Article scientifique
Anglais

Dermatopharmacokinetic prediction of topical drug bioavailability in vivo

Publié dansJournal of investigative dermatology, vol. 127, no. 4, p. 887-894
Date de publication2007
Résumé

The overall goal of this study was to explore the potential of using stratum corneum (SC) tape-stripping, post-application of a topical drug formulation, to derive dermatopharmacokinetic parameters describing the rate and extent of delivery into the skin. Ibuprofen was administered in 75:25 v/v propylene glycol-water to the ventral forearms of human volunteers for periods ranging between 15 and 180 minutes. Subsequently, SC was tape-stripped, quantified gravimetrically, and extracted for drug analysis. Together with concomitant transepidermal water loss measurements, SC concentration-depth profiles of the drug were reproducibly determined and fitted mathematically. The SC-vehicle partition coefficient (K) and a first-order rate constant related to ibuprofen diffusivity in the membrane (D/L2, where L=SC thickness) were derived from data-fitting and characterized the extent and rate of drug absorption across the skin. Integration of the concentration profiles yielded the total drug amount in the SC at the end of the application period. Using K and D/L2 obtained from the 30-minute exposure, it was possible to predict ibuprofen uptake as a function of time into the SC. Prediction and experiment agreed satisfactorily suggesting that objective and quantitative information, with which to characterize topical drug bioavailability, can be obtained from this approach.

Mots-clés
  • Absorption
  • Administration, Topical
  • Adult
  • Biological Availability
  • Epidermis/metabolism
  • Female
  • Forearm
  • Humans
  • Ibuprofen/administration & dosage/pharmacokinetics
  • Male
  • Middle Aged
  • Pharmacokinetics
  • Predictive Value of Tests
  • Skin/metabolism
  • Solutions
  • Surgical Tape
Citation (format ISO)
HERKENNE, Christophe et al. Dermatopharmacokinetic prediction of topical drug bioavailability in vivo. In: Journal of investigative dermatology, 2007, vol. 127, n° 4, p. 887–894. doi: 10.1038/sj.jid.5700642
Fichiers principaux (1)
Article (Published version)
accessLevelRestricted
Identifiants
ISSN du journal0022-202X
591vues
0téléchargements

Informations techniques

Création27.01.2011 14:43:00
Première validation27.01.2011 14:43:00
Heure de mise à jour14.03.2023 16:12:02
Changement de statut14.03.2023 16:12:02
Dernière indexation15.01.2024 22:04:55
All rights reserved by Archive ouverte UNIGE and the University of GenevaunigeBlack