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The Microsponge Delivery System of Itraconazole: Preparation, Characterization and Release Studies
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  • Journal title : KSBB Journal
  • Volume 26, Issue 3,  2011, pp.217-222
  • Publisher : Korean Society for Biotechnology and Bioengineering
  • DOI : 10.7841/ksbbj.2011.26.3.217
 Title & Authors
The Microsponge Delivery System of Itraconazole: Preparation, Characterization and Release Studies
Cho, Young-Ho; Lee, Jong-Hwa; Kim, Hak-Hyung; Lee, Gye-Won;
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Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. To improve the oral absorption and dissolution of poorly water-soluble itraconazole, microsponge system composed of E100 and polyvinyl alcohol(PVA) formulated by quasi-emulsion solvent diffusion method, and its physicochemical properties and pharmacokinetic parameters of itraconazole were studied. The microsponge of itraconazole were discrete free flowing micro sized particles with perforated orange peel like morphology as visualized by scanning electron microscope (SEM). Results showed that the drug loading efficiency, production yield, and particle size of itraconazole microsponge were affected by drug to polymer ratio, the volume of internal phase containing methylene chloride, stirring rate and the concentration of PVA used. Also, the results showed that the dissolution rate of itraconazole from the microsponges was affected by drug to polymer ratio. In other words, the release rate of itraconazole from microsponges was increased from at least 27.43% to 64.72% after 2 h. The kinetics of dissolution mechanism showed that the dissolution data followed Korsmeyer-Peppas model. Therefore, these results suggest that microsponge system can be useful for the oral delivery of itraconazole by manipulating the release profile.
microsponge;itraconazole; E 100;polymer;dissolution rate;
 Cited by
Fromtling, R. A. (1987) Recent Trends in the Discovery:Development and Evaluation of Antifungal Agents. pp. 233- 249. J. R. Prous Science Publishers, Barcelona, Spain.

Kapsi, S. G. and J. W. Ayres (2001) Processing factors in development of solid formulation itraconazole for enhancement of drug dissolution and bioavailability. Int. J. Pharm. 229: 193-203. crossref(new window)

Comoglu, T. and N. Gonul (2000) Microsponge Delivery Systems. J. Faculty Pharm. Ankara Univ. 29: 75-86.

Kislalioglu, M. S., M. A. Khan, C. Blount, R. W. Goettsch, and S. Bolton (1991) Physical characterization and dissolution properties of ibuprofen: udragit coprecipitates. J. Pharm. Sci. 80: 799-804. crossref(new window)

Jenquin, M. R. and J. W. Mc Ginity (1994) Characterization of acrylic resin matrix films and mechanisms of drug/polymer interactions. Int. J. Pharm. 101: 23-34. crossref(new window)

Comoglu, T. N. and T. Baykara (2002) The effects of pressure and direct compression on tab letting of microsponges. Int. J. Pharm. 242: 191-195. crossref(new window)

Comoglu, T., N. Gonill, and T. Baykara (2003) Preparation and in vitro evaluation of modified release ketoprofen microsponges. Il Farmaco 58: 101-106. crossref(new window)

Erdal, C., O. Mine, and A. Ahmet (2006) Design and evaluation of colon specific drug delivery system containing flurbiprofen microsponges.Int. J. Pharm. 318: 103-117. crossref(new window)

Kawashima, Y., T. Iwamoto, T. Niwa, H. Takeuchi, and T. Hino (1993) Role of the solvent-diffusion-rate modifier in a new emulsion solvent diffusion method for preparation of ketoprofen microspheres. J. Microencapsul. 10: 329-340. crossref(new window)

Kawashima, Y., T. Niwa, N. Takeuchi, T. hino, and Y. Ito (1992) Control of prolonged drug release and compression properties of ibuprofen microsponge with acrylic polymer, Eudragit RS, by changing their interparticle porosity. Chem. Pharm. Bull. 40: 196-201. crossref(new window)

Barkai, A., Y. V. Pathak, and S. Benita (1990). Polyacrylate (Eudragit retard) microspheres for oral controlled release of nifedipine. I. Formulation design and process optimization. Drug Develop. Ind. Pharm. 16: 2057-2075. crossref(new window)

Pongpaibul, Y., J. C. Price, and C. W. Whitworth (1984) Preparation and evaluation of controlled release indomethacin microspheres. Drug Develop. Ind. Pharm. 10: 1597-1616. crossref(new window)

Nokhodchi, A., M. Jelvehgari, M. R. Siahi, and M. R. Mozafari (2007) Factors affecting the morphology of benzoyl peroxide microsponges. Micron. 38: 834-840. crossref(new window)

Jelvehgari, M., M. R. Siahi-Shadbad, S. Azarmi, G. P. Martin, and A. Nokhodchi (2006) The microsponge delivery system of benzoyl peroxide: Preparation, characterization and release studies. Int. J. Pharm. 308: 124-132. crossref(new window)

Yang, M.S., F. D. Cui, B. G. You, Y. L. Fan, L. Wang, P. Yue, and H. Yang (2003) Preapration of sustined-release nifedipine microspheres with Eudragit RS and Aerosil using quasiemulsion solvent diffusion method. Int. J. Pharm. 259: 103-113. crossref(new window)

Siepmann, J. and N. A. Peppas (2001) Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv. Drug Deli. Rev. 48: 139-157. crossref(new window)