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Scientific article
English

Dermatopharmacokinetic prediction of topical drug bioavailability in vivo

Contributors

Herkenne, Christophe; Naik, Aarti; Kalia, Yogeshvar; Hadgraft, Jonathan; Guy, Richard H.

Published in

Journal of investigative dermatology, vol. 127, no. 4, p. 887-894

Publication date

2007

Abstract

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.

Keywords

  • 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

UNIGE affiliation entities

Citation (ISO format)

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

Main files (1)

Article (Published version)

Identifiers

Journal ISSN

0022-202X
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Technical informations

Creation

27/01/2011 14:43:00

First validation

27/01/2011 14:43:00

Update

14/03/2023 16:12:02

Status update

14/03/2023 16:12:02

Last indexation

29/10/2024 17:44:39
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