UNIGE document Scientific Article
previous document  unige:14232  next document
add to browser collection
Title

Dermatopharmacokinetic prediction of topical drug bioavailability in vivo

Authors
Hadgraft, Jonathan
Published in Journal of Investigative Dermatology. 2007, vol. 127, no. 4, p. 887-94
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 AbsorptionAdministration, TopicalAdultBiological AvailabilityEpidermis/metabolismFemaleForearmHumansIbuprofen/administration & dosage/pharmacokineticsMaleMiddle AgedPharmacokineticsPredictive Value of TestsSkin/metabolismSolutionsSurgical Tape
Stable URL http://archive-ouverte.unige.ch/unige:14232
Full text
Article (Published version) (221 Kb) - document accessible for UNIGE members only Limited access to UNIGE
Identifiers
PMID: 17139266
Structures

154 hits

3 downloads

Update

Deposited on : 2011-01-28

Export document
Format :
Citation style :