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The Korean Society for Biotechnology and Bioengineering (한국생물공학회)
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The Microsponge Delivery System of Itraconazole: Preparation, Characterization and Release Studies

이트라코나졸 마이크로스폰지의 약물 전달 시스템: 제조, 특성 및 방출 연구

  • Cho, Young-Ho (Department of Pharmaceutical Engineering, Konyang University) ;
  • Lee, Jong-Hwa (Division of Research and Development, Korea Institute of Toxicology) ;
  • Kim, Hak-Hyung (Department of Pharmaceutical Engineering, Konyang University) ;
  • Lee, Gye-Won (Department of Pharmaceutical Engineering, Konyang University)
  • 조영호 (건양대학교 제약공학과) ;
  • 이종화 (한국화학연구원 안전성 평가 연구소) ;
  • 김학형 (건양대학교 제약공학과) ;
  • 이계원 (건양대학교 제약공학과)
  • Received : 2011.03.28
  • Accepted : 2011.05.24
  • Published : 2011.06.30
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Abstract

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 $Eudragit^{(R)}$ 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.

Keywords

References

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