Effects of penetration enhancers on in vitro percutaneous absorption of low molecular weight heparin through human skin

Glen Xiong, Danyi Quan, Howard I. Maibach

Research output: Contribution to journalArticle

27 Scopus citations

Abstract

The influence of the penetration enhancers, laurocapram (Azone®), 1,8-cineole, and nerolidol on the in vitro percutaneous absorption of low molecular weight heparin (LMWH) through human skin was investigated. The enhancing effectiveness of the enhancers decreased in the order: laurocapram > nerolidol, 1,8-cineole. Compared to the control formulation (without enhancers), a 4.4-fold enhancement was observed with 2% laurocapram and a 2-fold enhancement resulted with 2% nerolidol. There were no significant promoting effects at low concentrations of 1,8-cineole; however, a 3.5-fold increase in LMWH flux resulted with 10% 1,8-cineole. The highest enhancement factor was 5.6 with 5% laurocapram. Cellophane tape-stripping of the stratum corneum did not affect drug flux compared to the control (full-thickness skin). Thus the epidermis and dermis, as well as the stratum corneum, may constitute major rate determining barriers for LMWH permeation across human skin.

Original languageEnglish (US)
Pages (from-to)289-296
Number of pages8
JournalJournal of Controlled Release
Volume42
Issue number3
DOIs
StatePublished - Dec 1996

Keywords

  • 1,8-Cineole
  • Laurocapram
  • Low molecular weight heparin
  • Nerolidol
  • Penetration enhancer
  • Percutaneous absorption

ASJC Scopus subject areas

  • Pharmaceutical Science

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