In vitro penetration through the skin layers of topically applied glucocorticoids

Drug Test Anal. 2018 Oct;10(10):1528-1535. doi: 10.1002/dta.2412. Epub 2018 Jun 20.

Abstract

Corticoids are actives widely used in the treatment of skin diseases. This work aims to study the penetration of 3 corticoids (betamethasone, clobetasol, and flurandrenolide), their relationship with their Log D values and the effects of the vehicles. The 3 compounds were applied on a Franz-type diffusion cell in propylene glycol solution and their respective commercial creams and ointments. The active amounts found in the stratum corneum, epidermal, and dermal layers of the skin were investigated. Their diffusions were greatly affected by the formulation; moreover higher amounts of substance in the epidermis and dermis were detected in ointments than in creams. The enhancement effect of propylene glycol was also observed. The differences between the 3 substances could be related to their lipophilicity, molecular structure, and molecular weight. The more hydrophobic compounds (clobetasol and betamethasone) are present in higher amounts in the epidermis and dermis, while the hydrophilic compound (flurandrenolide) is mostly present in the receptor fluid.

Keywords: clobetasol; corticosteroids; flurandrenolide; percutaneous absorption; propylene glycol.

MeSH terms

  • Administration, Topical
  • Animals
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / pharmacokinetics*
  • Betamethasone / administration & dosage
  • Betamethasone / pharmacokinetics*
  • Clobetasol / administration & dosage
  • Clobetasol / pharmacokinetics*
  • Flurandrenolone / administration & dosage
  • Flurandrenolone / pharmacokinetics*
  • Glucocorticoids / administration & dosage
  • Glucocorticoids / pharmacokinetics*
  • Humans
  • Pharmaceutical Vehicles / chemistry
  • Skin / metabolism
  • Skin Absorption*
  • Swine

Substances

  • Anti-Inflammatory Agents
  • Glucocorticoids
  • Pharmaceutical Vehicles
  • Flurandrenolone
  • Betamethasone
  • Clobetasol