In vitro evaluation of a series of azone analogs as dermal penetration enhancers: III. Acyclic amides

B. B. Michniak, M. R. Player, L. C. Fuhrman, C. A. Christensen, J. M. Chapman, J. W. Sowell

Research output: Contribution to journalArticlepeer-review

22 Scopus citations

Abstract

A scries of acyclic amides was synthesized and tested for enhancement properties using excised hairless mouse skin and hydrocortisone 21-acetate as the model drug. All compounds were applied at 0.4 M (or at their respective saturation solubilities) in propylene glycol. Azone (0.4 M) was used as a standard enhancer. Enhancement ratios were calculated for flux, 24 h diffusion cell receptor concentrations (Q24) and 24 h full-thickness mouse skin steroid content. Enhancer 5 showed the highest activity for flux (35.22-fold over control), 24 h receptor concentration (79.86-fold over control) and skin drug content (4.3-fold over control). These enhancement ratios were higher than those for Azone which were 19.51, 38.30 and 1.5-fold over control, respectively. Enhancers 4, 10 and 11 showed similar Q24 values to Azone, and 3, 9 and 10 increased skin steroid content to a greater extent than Azone.

Original languageEnglish (US)
Pages (from-to)231-239
Number of pages9
JournalInternational Journal of Pharmaceutics
Volume110
Issue number3
DOIs
StatePublished - Sep 26 1994
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Keywords

  • Amide
  • Azone analog
  • Flux
  • Hairless mouse
  • Hydrocortisone 21-acetate
  • Percutaneous absorption
  • Skin retention

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