Stability of sulforaphane for topical formulation

Stephen J. Franklin, Sally E Dickinson, Kelly L. Karlage, G. T. Bowden, Paul B Myrdal

Research output: Contribution to journalArticle

24 Citations (Scopus)

Abstract

Context: Sulforaphane (SFN) is a natural compound that has been investigated as a chemopreventive agent. SFN has been shown to inhibit the activator-protein-1 (AP-1) transcription factor and may be effective for inhibition of ultraviolet (UV) induced skin carcinogenesis. This study was designed to investigate the stability of SFN as a function of pH, temperature and in various solvents and formulations. Materials and methods: Stability was analyzed using high-performance liquid chromatography. A potential lead formulation was identified and evaluated in vivo. Results: SFN was determined to undergo apparent first-order degradation kinetics for the conditions explored. It was observed that SFN undergoes base catalyzed degradation. Buffer species and solvent type impacts stability as well. SFN was found to be very sensitive to temperature with degradation rate changing by a factor of nearly 3.1 for every 10°C change in temperature (at pH 4.0). SFN completely degraded after 30 days in a conventional pharmaceutical cream formulation. Improved stability was observed in organic formulation components. Stability studies were conducted on two nonaqueous topical formulations: a polyethylene glycol (PEG) ointment base and an organic oleaginous base. Conclusion: Topically applied SFN in the PEG base formulation significantly reduced AP-1 activation after UV stimulation in the skin of a transgenic mouse model, indicating that SFN in this formulation retains efficacy in vivo.

Original languageEnglish (US)
Pages (from-to)494-502
Number of pages9
JournalDrug Development and Industrial Pharmacy
Volume40
Issue number4
DOIs
StatePublished - Apr 2014

Fingerprint

Transcription Factor AP-1
Degradation
Temperature
Skin
Ointment Bases
sulforafan
Drug Compounding
High performance liquid chromatography
Transgenic Mice
Buffers
Carcinogenesis
Transcription Factors
Chemical activation
High Pressure Liquid Chromatography
Kinetics
Pharmaceutical Preparations
Lead

Keywords

  • Activator-protein-1
  • Base catalysis
  • Degradation
  • Hydrolysis
  • in vivo
  • Isothiocyanate
  • UVB

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology
  • Organic Chemistry

Cite this

Stability of sulforaphane for topical formulation. / Franklin, Stephen J.; Dickinson, Sally E; Karlage, Kelly L.; Bowden, G. T.; Myrdal, Paul B.

In: Drug Development and Industrial Pharmacy, Vol. 40, No. 4, 04.2014, p. 494-502.

Research output: Contribution to journalArticle

Franklin, Stephen J. ; Dickinson, Sally E ; Karlage, Kelly L. ; Bowden, G. T. ; Myrdal, Paul B. / Stability of sulforaphane for topical formulation. In: Drug Development and Industrial Pharmacy. 2014 ; Vol. 40, No. 4. pp. 494-502.
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