Phase behavior of itraconazole-phenol mixtures and its pharmaceutical applications

Chun Woong Park, Heidi M. Mansour, Tack Oon Oh, Ju Young Kim, Jung Myung Ha, Beom Jin Lee, Sang Cheol Chi, Yun Seok Rhee, Eun Seok Park

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

The aims of this study were to examine the phase behavior of itraconazole-phenol mixtures and assess the feasibility of topical formulations of itraconazole using eutectic mixture systems. Itraconazole-phenol eutectic mixtures were characterized using differential scanning calorimetry, Fourier transform infrared spectroscopy, 1H-nuclear magnetic resonance, and powder X-ray diffractometry. The skin permeation rates of itraconazole-phenol eutectic formulations were determined using Franz diffusion cells fitted with excised hairless mouse skins. Itraconazole can form eutectic compounds with phenol, and the hydrogen-bonding interactions between the carbonyl group in the itraconazole and hydroxyl group in phenol play a major role in itraconazole-phenol eutectic formation. Despite its high molecular weight and hydrophobicity, the drug (i.e.; itraconazole) can be permeated through excised hairless mouse skins from itraconazole-phenol eutectic formulations. The findings of this study emphasize the capabilities of the topical application of itraconazole via external preparations.

Original languageEnglish (US)
Pages (from-to)652-658
Number of pages7
JournalInternational Journal of Pharmaceutics
Volume436
Issue number1-2
DOIs
StatePublished - Oct 15 2012
Externally publishedYes

Keywords

  • Eutectic mixture
  • Itraconazole
  • Phenol
  • Skin permeation
  • Topical

ASJC Scopus subject areas

  • Pharmaceutical Science

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