Enhanced solubility and oral bioavailability of itraconazole by combining membrane emulsification and spray drying technique

Choi, Young Keun, Poudel, Bijay K., Marasini, Nirmal, Yang, Kwan Yeol, Kim, Jeong Whan, Kim, Jong Oh, Choi, Han-Gon and Yong, Chul Soon (2012) Enhanced solubility and oral bioavailability of itraconazole by combining membrane emulsification and spray drying technique. International Journal of Pharmaceutics, 434 1-2: 264-271. doi:10.1016/j.ijpharm.2012.05.039


Author Choi, Young Keun
Poudel, Bijay K.
Marasini, Nirmal
Yang, Kwan Yeol
Kim, Jeong Whan
Kim, Jong Oh
Choi, Han-Gon
Yong, Chul Soon
Title Enhanced solubility and oral bioavailability of itraconazole by combining membrane emulsification and spray drying technique
Journal name International Journal of Pharmaceutics   Check publisher's open access policy
ISSN 0378-5173
1873-3476
Publication date 2012-09-15
Year available 2012
Sub-type Article (original research)
DOI 10.1016/j.ijpharm.2012.05.039
Open Access Status Not Open Access
Volume 434
Issue 1-2
Start page 264
End page 271
Total pages 8
Place of publication Amsterdam, Netherlands
Publisher Elsevier BV
Language eng
Formatted abstract
The objective of the present study was to enhance solubility and bioavailability of itraconazole by a combined use of membrane emulsification and spray drying solidification technique. A shirasu-porous-glass (SPG) membrane with a mean pore size of 2.5 μm was used to produce monodispersed microemulsions of itraconazole consisting of methylene chloride as the dispersed phase, a mixture of Transcutol HP and Span 20 as a stabilizer, and dextran as solid carrier dissolved in water as the continuous phase. The dispersed phase permeated through the SPG membrane into the continuous phase at an agitator speed of 150 rpm, a feed pressure of 15 kPa and a continuous phase temperature of 25 °C and the resultant emulsion was solidified using spray-drying technique. Solid state characterizations of the solid emulsion showed that the crystal state of itraconazole in solid emulsion was converted from crystalline to amorphous form. The solid emulsion of itraconazole displayed a significant increase in the dissolution rate than that of pure itraconazole. Furthermore, the solid emulsion after oral administration gave about eight-fold higher AUC and about ten-fold higher Cmax in rats than pure itraconazole powder (p < 0.05), indicating this formulation greatly improved the oral bioavailability of drug in rats. Thus, these results demonstrated that the SPG membrane emulsification system combined with spray-drying technique could be used as a promising technique to develop solid formulation of itraconazole with enhanced solubility and bioavailability.
Keyword Bioavailability
Itraconazole
Membrane emulsification
Solubility
Spray-drying
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Chemistry and Molecular Biosciences
 
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