Effect of /-Menthol on the Permeation of Indomethacin, Mannitol and Cortisone through Excised Hairless Mouse Skin

Masawo Kakemi, Kazunori Katayama, Tamotsu Koizumi, Osamu Takahashi, Rakan Matsui, Setsuko Morigaki, Tetsuya Aiba

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

The effect of /-menthol on the skin permeability of mannitol, cortisone or indomethacin was examined by an in vitro penetration technique with hairless mouse skin. The donor solution was prepared with phosphate buffered saline, ethanol: buffered saline (20:80, v/v) or ethanol: buffered saline (20:80, v/v) containing 1% (w/v) /-menthol. Although ethanol showed little enhancing effect, /-menthol in an aqueous ethanol vehicle at pH 7.4 increased the permeability coefficients of mannitol and indomethacin by about 100 times that of the control (an aqueous vehicle) and increased that of cortisone by about 10 times. /-Menthol, however, scarcely enhanced the penetration of indomethacin at pH 3.0, the majority of the species being in unionized form. These results suggested that the menthol-ethanol-aqueous system enhanced skin permeability through a direct effect on the polar and/or lipid pathways, while the thermodynamic activity of the penetrant molecule in the delivery vehicle might also influence the effectiveness of the penetration enhancer.

Original languageEnglish
Pages (from-to)3097-3099
Number of pages3
JournalChemical and Pharmaceutical Bulletin
Volume40
Issue number11
DOIs
Publication statusPublished - Jan 1 1992
Externally publishedYes

Keywords

  • /-menthol
  • cortisone
  • hairless mouse
  • indomethacin
  • mannitol
  • penetration enhancer
  • skin permeability

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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