title: Amidated pectin-based wafers for econazole buccal delivery: formulation optimization and antimicrobial efficacy estimation.
abstract: Combinations of low-methoxy amidated pectin (LMAP) and carboxymethylcellulose (CMC) were used to develop a lyophilized wafer formulation, aimed to obtain prolonged residence and controlled release of econazole nitrate (ECN) in the oral cavity. Ternary ECN/sulphobutylether-ß-cyclodextrin/citric acid complex, resulted as the most efficient system against selected Candida strains, was loaded into this formulation. The final product with the desired and predicted quality was developed by an experimental design strategy. The experimental values of mucoadhesion strength (28.37 ± 0.04 mg/cm(2)) and residence time (88.1 ± 0.1 min) obtained for the optimized wafer formulation were very close to the predicted ones, thus demonstrating the actual reliability and usefulness of the assumed model in the preparation of buccal wafers. The optimized formulation provided a constant ECN in situ release of 5mg/h and was efficacious against selected Candida strains in vitro. This clearly proved its potential as a novel effective delivery system for the therapy of oral candidiasis.
authors: Department of Chemistry, School of Human Health Sciences, University of Florence, Via Schiff 6, Sesto Fiorentino I-50019, Florence, Italy.
authors: Paola
authors: P
authors: Mura
authors: Department of Chemistry, School of Human Health Sciences, University of Florence, Via Schiff 6, Sesto Fiorentino I-50019, Florence, Italy.
authors: Natascia
authors: N
authors: Mennini
authors: Department of Microbiology, Faculty of Pharmacy and Biochemistry, University of Zagreb, Schrotova 39, Zagreb, Croatia.
authors: Ivan
authors: I
authors: Kosalec
authors: Department of Chemistry, School of Human Health Sciences, University of Florence, Via Schiff 6, Sesto Fiorentino I-50019, Florence, Italy.
authors: Sandra
authors: S
authors: Furlanetto
authors: Department of Chemistry, School of Human Health Sciences, University of Florence, Via Schiff 6, Sesto Fiorentino I-50019, Florence, Italy.
authors: Serena
authors: S
authors: Orlandini
authors: Department of Pharmaceutical Technology of Pharmacy and Biochemistry, University of Zagreb, A. Kovačića 1, Zagreb, Croatia. Electronic address: mjug@pharma.hr.
authors: Mario
authors: M
authors: Jug
mesh_terms: D000269:Adhesives / Q000737:chemistry; D000577:Amides / Q000737:chemistry; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects*; D004337:Drug Carriers / Q000737:chemistry; D004464:Econazole / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D009061:Mouth Mucosa / Q000187:drug effects*; D010368:Pectins / Q000737:chemistry*; D013552:Swine
chemical_list: D000269:Adhesives; D000577:Amides; D000935:Antifungal Agents; D004337:Drug Carriers; D004464:Econazole; D010368:Pectins
keywords: Buccal wafer; Econazole nitrate; Experimental design; Low methoxy amidated pectin; Mucoadhesion; Sulphobutylether-ß-cyclodextrin