Phase solubility and inclusion complex of itraconazole with β-cyclodextrin using supercritical carbon dioxide

Ali H. Al-Marzouqi, Ibrahim Shehatta, Baboucarr Jobe, Ali Dowaidar

Research output: Contribution to journalArticlepeer-review

81 Citations (Scopus)

Abstract

Phase-solubility techniques were used to assess the formation of inclusion complex between itraconazole and β-cyclodextrin. The stability constant and free energies of transfer of itraconazole from aqueous solution to the cavity of β-cyclodextrin were calculated. Itraconazole solubility in supercritical carbon dioxide (SC CO2) was measured at different temperatures and pressures. Drug formulations of itraconazole were prepared by complexation of the drug into β-cyclodextrin using SC CO2. Effects of temperature and pressure on inclusion yield of the prepared complexes were studied. The solvent-free inclusion complexes obtained from this method were characterized by UV spectroscopy, differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy and compared to those obtained from physical mixing and coprecipitation methods. Results showed that β-cyclodextrin significantly improved solubility of itraconazole in aqueous solutions. The free energies of transfer of itraconazole from aqueous solution to the cavity of β-cyclodextrin increased negatively with increasing β-cyclodextrin concentration. Higher inclusion yields were obtained in the SC CO2 method compared to physical mixing and coprecipitation methods. Both temperature and pressure had significant effects on itraconazole solubility in SC CO2 and the inclusion yield of the complex prepared by SC CO2 method.

Original languageEnglish
Pages (from-to)292-304
Number of pages13
JournalJournal of Pharmaceutical Sciences
Volume95
Issue number2
DOIs
Publication statusPublished - Feb 2006

Keywords

  • Cyclodextrin
  • Inclusion complex
  • Itraconazole
  • Solubility
  • Stability
  • Supercritical carbon dioxide

ASJC Scopus subject areas

  • Pharmaceutical Science

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