Improved solubility of ketoconazole and its activity against Candida species by ketoconazole:β-cyclodextrin:proline complexation

A. BRUNO; V. AIASSA; A. ZOPPI; M. LONGHI

Rosario

Congreso; 4a Reunión Internacional de Ciencias Farmacéuticas (RiCIFA).; 2016

Universidad Nacional de Rosario

Ketoconazole (KET) is an antifungal agent suitable for the treatment of candidiasis and other systemic fungal infections. The major drawback in the therapeutic efficacy of KET is its very low aqueous solubility because of its hydrophobic structure. Cyclodextrins have been used to improve the poor aqueous solubility of these drugs. On the other hand, the antimicrobial activity of nitric oxide (NO) against a wide array of microorganisms is well documented resulting and synergistic with azoles. As proline (PRO) is considered a NO source, the objective of this work was to assess the effect of ternary complex formation KET: βCD: PRO in the solubility and antifungal activity of KET.