Effect of propylene glycol on ibuprofen absorption into human skin in vivo

C Herkenne, A Naik, Y N Kalia, J Hadgraft, R H Guy

Research output: Contribution to journalArticle

59 Citations (Scopus)

Abstract

The objective was to assess the impact of propylene glycol (PG), a common cosolvent in topical formulations, on the penetration of ibuprofen into human skin in vivo. Drug uptake into the stratum corneum (SC), following application of saturated formulations containing from 0 to 100% v/v PG, was assessed by tape-stripping. Dermatopharmacokinetic parameters, characterizing drug amount in and diffusivity through the SC, were derived. The solubility behavior of ibuprofen in PG-water mixtures was carefully evaluated, as were a number of other physical properties. Ibuprofen delivery depended on the level of PG in the vehicle, despite all formulations containing the drug at equal thermodynamic activity. PG appeared to alter the solubility of ibuprofen in the SC (presumably via its own uptake into the membrane), the effect becoming more important as the volume fraction of cosolvent in the formulation increased. In summary, tape-stripping experiments, with careful interpretation, can reveal details of a drug's bioavailability in the skin following topical application and may be used to probe the mechanism(s) by which certain excipients influence local drug delivery
Original languageEnglish
Pages (from-to)185-197
Number of pages13
JournalJournal of Pharmaceutical Sciences
Volume97
Issue number1
DOIs
Publication statusPublished - Jan 2008

Keywords

  • Skin
  • Solubility
  • Percutaneous absorption
  • Dermatopharmacokinetics
  • Diffusivity
  • Partition coefficient
  • Topical drug bioavailability

Fingerprint Dive into the research topics of 'Effect of propylene glycol on ibuprofen absorption into human skin in vivo'. Together they form a unique fingerprint.

  • Cite this