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, (1)H-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.
authors.affiliation: School of Pharmacy, Sungkyunkwan University, 300 Cheoncheon-dong, Jangan-gu, Suwon, Gyeonggi-do 440-746, Republic of Korea.
authors.forename: Chun-Woong
authors.initials: CW
authors.lastname: Park
authors.forename: Heidi M
authors.initials: HM
authors.lastname: Mansour
authors.forename: Tack-Oon
authors.initials: TO
authors.lastname: Oh
authors.forename: Ju-Young
authors.initials: JY
authors.lastname: Kim
authors.forename: Jung-Myung
authors.initials: JM
authors.lastname: Ha
authors.forename: Beom-Jin
authors.initials: BJ
authors.lastname: Lee
authors.forename: Sang-Cheol
authors.initials: SC
authors.lastname: Chi
authors.forename: Yun-Seok
authors.initials: YS
authors.lastname: Rhee
authors.forename: Eun-Seok
authors.initials: ES
authors.lastname: Park
mesh_terms: D000818:Animals; D066298:In Vitro Techniques; D017964:Itraconazole / Q000737:chemistry* / Q000378:metabolism; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D008813:Mice, Inbred ICR; D019800:Phenol / Q000737:chemistry* / Q000378:metabolism; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
chemical_list: D017964:Itraconazole; D019800:Phenol