Simultaneous improvement of ketoconazole solubility, antifungal and antibiofilm activity by multicomponent complexation

摘要

Background:A novel multicomponent complex (MC) of ketoconazole (KET) with beta-cyclodextrin (beta-CD) andN-acetylcysteine (NAC) was developed with the purpose of improving the solubility as well as the antifungal and antibiofilm activity of KET againstCandida albicans.Results & methodology:The interactions among the components were studied using nuclear magnetic resonance, thermal analysis, powder x-ray diffraction, infrared spectroscopy and scanning electron microscopy. Phase-solubility studies demonstrated a considerable increase in the solubility of the MC. An enhancement in antibiofilm and antifungal activity of MC was determined againstC. albicansby XTT assay and microbiological studies.Conclusion:This MC, with improvements in the drug pharmaceutical performance, might have an important potential in the development of new pharmaceutical formulations of KET.