title: Clotrimazole nanoparticle gel for mucosal administration.
abstract: In this study a formulation suitable to be applied on oral and/or vaginal mucosa has been developed for the treatment of fungal infections. The aim of the research is a comparison between clotrimazole (CLO) containing semisolid formulations based on monoolein aqueous dispersion (MAD) or nanostructured lipid carrier (NLC). MAD and NLC have been characterized in terms of morphology and dimensional distribution by cryogenic Transmission Electron Microscopy (cryo-TEM) and Photon Correlation Spectroscopy (PCS). CLO was encapsulated with high entrapment efficiency both in MAD and in NLC, according to Sedimentation Field Flow Fractionation (SdFFF) combined with HPLC. CLO recovery in MAD and NLC has been investigated by time. In order to obtain formulations with suitable viscosity for mucosal application, MAD was diluted with a carbomer gel, while NLC was directly viscosized by the addition of poloxamer 407 in the dispersion. The rheological properties of MAD and NLC after viscosizing have been investigated. Franz cell has been employed to study CLO diffusion from the different vehicles, evidencing diffusion rates from MAD and NLC superimposable to that obtained using Canesten(®). An anticandidal activity study demonstrated that both CLO-MAD and CLO-NLC were more active against Candida albicans with respect to the pure drug.
authors.affiliation: Department of Pharmaceutical Sciences, University of Ferrara, I-44121 Ferrara, Italy. ese@unife.it
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Esposito
authors.affiliation: Department of Pharmaceutical Sciences, University of Ferrara, I-44121 Ferrara, Italy.
authors.forename: Laura
authors.initials: L
authors.lastname: Ravani
authors.affiliation: Department of Chemistry, University of Ferrara, Ferrara, Italy.
authors.forename: Catia
authors.initials: C
authors.lastname: Contado
authors.affiliation: Department of Pharmaceutical Sciences, University of Ferrara, I-44121 Ferrara, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Costenaro
authors.affiliation: Macromolecular Chemistry II, University of Bayreuth, Germany.
authors.forename: Markus
authors.initials: M
authors.lastname: Drechsler
authors.affiliation: Department of Biology and Evolution, LT Terra&Acqua Tech UR7, University of Ferrara, Ferrara, Italy.
authors.forename: Damiano
authors.initials: D
authors.lastname: Rossi
authors.affiliation: Department of Pharmaceutical Sciences, University of Ferrara, I-44121 Ferrara, Italy.
authors.forename: Enea
authors.initials: E
authors.lastname: Menegatti
authors.affiliation: Department of Biology and Evolution, LT Terra&Acqua Tech UR7, University of Ferrara, Ferrara, Italy.
authors.forename: Alessandro
authors.initials: A
authors.lastname: Grandini
authors.affiliation: Department of Pharmaceutical Sciences, University of Ferrara, I-44121 Ferrara, Italy.
authors.forename: Rita
authors.initials: R
authors.lastname: Cortesi
mesh_terms: D058956:Administration, Mucosal; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects; D003022:Clotrimazole / Q000737:chemistry* / Q000494:pharmacology; D004058:Diffusion; D004337:Drug Carriers / Q000737:chemistry; D005782:Gels / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D012212:Rheology; D014783:Viscosity
chemical_list: D000935:Antifungal Agents; D004337:Drug Carriers; D005782:Gels; D020442:Poloxamer; D003022:Clotrimazole