Sertaconazole-Loaded Cyclodextrin–Polysaccharide Hydrogels as Antifungal Devices§

Abstract

The aim of the present work was to develop novel hydrogels for delivering sertaconazole based on cyclodex- trins and various biocompatible polysaccharides. Sertaconazole is an antifungal agent very effective for treatment of Can- dida albicans infections. However its poor aqueous solubility is still a challenging issue for developing suitable formula- tions. Complexation with cyclodextrins is a very attractive route to overcome this limitation, simultaneously enhancing its antifungal effectiveness. Hydroxypropyl--cyclodextrin (HPCD) hydrogels prepared by direct cross-linking in presence of methylcellulose (MC), hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC), carboxymethyl cellu- lose (CMCNa), or dextran were transparent and swelled in water without dissolving, which enables the formation of mi- croenvironments very rich in cyclodextrin cavities responsible for hosting the drug and control its release rate. HP CD hydrogels showed a high capability to load sertaconazole (with partition coefficients from 22 to 470) while still combining high water affinity (superabsorbency), versatile biomechanical properties (hardness and compressibility) and sustained re- lease behavior (up to 4 days). Importantly, sertaconazol-loaded hydrogels showed effectiveness against Candida albicans in culture medium. HPCD-polysaccharide hydrogels could be useful as sertaconazole delivery systems for the treatment of mucosal infections.