Azone analogues as penetration enhancers: effect of different vehicles on hydrocortisone acetate skin permeation and retention

B. B. Michniak, M. R. Player, J. M. Chapman, J. W. Sowell

Research output: Contribution to journalArticlepeer-review

46 Scopus citations

Abstract

The permeation and skin retention of hydrocortisone-21 -acetate in hairless mouse skin in vitro was examined following topical pretreatment with four novel enhancers in four vehicles: isopropyl myristate (IPM), N-methyl-2-pyrrolidinone, (MP), polyethylene glycol 400 (PEG), and caprylic/capric/linoleic triglyceride (CT, Miglyol 818®). Controls included no vehicle pretreatment and vehicle pretreatment one hour prior to drug application to the skin. The standard enhancer studied was Azone. With enhancer 1 [N-(1-oxododecyl)morpholine], the rank order for 24 hour cumulative receptor steroid concentrations Q24 (μM) was PEG > IPM > MP/CT; for enhancer 2 [N-dodecyl-2-piperidinone]: PEG > IPM/MP/CT; for enhancer 3 [N-dodecyl-2-pyrrolidinone]: MP > CT/PEG/IPM; for enhancer 4 [N-(1-oxotetradecyl)hexahydro-2-oxo-1H-azepine]: PEG/MP/IPM > CT. For Q24 controls, one hour pretreatment with vehicles alone, rank order was IPM > MP/CT > PEG. Coadministration of the steroid with enhancer 2 with PEG or with propylene glycol reduced enhancer effectiveness compared to pretreatment with vehicle alone.

Original languageEnglish (US)
Pages (from-to)147-154
Number of pages8
JournalJournal of Controlled Release
Volume32
Issue number2
DOIs
StatePublished - Dec 1 1994
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Keywords

  • Azone
  • Enhancers
  • Hairless mouse skin
  • Skin permeation
  • Skin retention
  • Steroid
  • Vehicles

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