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

doi:10.1016/j.ijpharm.2012.07.054

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 journal › Article › peer-review

33 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 language	English (US)
Pages (from-to)	652-658
Number of pages	7
Journal	International Journal of Pharmaceutics
Volume	436
Issue number	1-2
DOIs	https://doi.org/10.1016/j.ijpharm.2012.07.054
State	Published - Oct 15 2012
Externally published	Yes

Keywords

Eutectic mixture
Itraconazole
Phenol
Skin permeation
Topical

ASJC Scopus subject areas

Pharmaceutical Science

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10.1016/j.ijpharm.2012.07.054

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title = "Phase behavior of itraconazole-phenol mixtures and its pharmaceutical applications",

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.",

keywords = "Eutectic mixture, Itraconazole, Phenol, Skin permeation, Topical",

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

note = "Funding Information: This study was supported by a grant of the Korean Health Technology R&D Project, Ministry for Health, Welfare & Family Affairs, Republic of Korea ( A092018 ). ",

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doi = "10.1016/j.ijpharm.2012.07.054",

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AU - Park, Chun Woong

AU - Mansour, Heidi M.

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AU - Ha, Jung Myung

AU - Lee, Beom Jin

AU - Chi, Sang Cheol

AU - Rhee, Yun Seok

AU - Park, Eun Seok

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N2 - 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.

AB - 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.

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Phase behavior of itraconazole-phenol mixtures and its pharmaceutical applications

Abstract

Keywords

ASJC Scopus subject areas

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