Effect of Different Skin Penetration Promoters in Halobetasol Propionate Permeation and Retention in Human Skin

Int J Mol Sci. 2017 Nov 21;18(11):2475. doi: 10.3390/ijms18112475.

Abstract

Halobetasol propionate (HB) is a potent synthetic corticosteroid used against inflammatory skin diseases, such as dermatitis, eczema, and psoriasis, among others. The aim of this study is to define how the presence of different skin penetration enhancers (nonane, menthone, limonene, azone, carene, decanol, linoleic acid and cetiol) affects the penetration and retention in skin of HB. To determine drug penetration through skin, 5% of each promoter was used in an ex vivo system with human skin on Franz cells. The results showed that the highest permeation occurs in the presence of menthone, followed by nonane. Permeation parameters were determined. The in vivo test was assessed, and the formulation containing HB-menthone presented better anti-inflammatory efficacy. These results are useful to generate a specific treatment according to each patient's needs, and the inflammatory characteristics of the disease.

Keywords: halobetasol propionate; permeation enhancers; skin inflammation; skin permeation; topical corticosteroid.

MeSH terms

  • Administration, Cutaneous
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / pharmacokinetics
  • Anti-Inflammatory Agents / pharmacology
  • Chromatography, High Pressure Liquid
  • Clobetasol / administration & dosage
  • Clobetasol / analogs & derivatives*
  • Clobetasol / pharmacokinetics
  • Clobetasol / pharmacology
  • Humans
  • Permeability / drug effects
  • Reproducibility of Results
  • Skin Absorption / drug effects*

Substances

  • Anti-Inflammatory Agents
  • halobetasol
  • Clobetasol