Amidated pectin-based wafers for econazole buccal delivery: Formulation optimization and antimicrobial efficacy estimation. (5th May 2015)

• Record Type: Journal Article
• Authors: Mura, Paola; Mennini, Natascia; Kosalec, Ivan; Furlanetto, Sandra; Orlandini, Serena; Jug, Mario
• Is Part Of: Carbohydrate polymers. Volume 121(2015)
• Page Start: 231
• Page End: 240
• Publication Date: 2015-05-05
• Subjects: Econazole nitrate -- Sulphobutylether-ß-cyclodextrin -- Low methoxy amidated pectin -- Experimental design -- Buccal wafer -- Mucoadhesion; Polysaccharides -- Periodicals; Polysaccharides -- Periodicals; Polysaccharides -- Périodiques; Electronic journals; 547.78
• DOI: 10.1016/j.carbpol.2014.11.065
• Languages: English
• ISSNs: 0144-8617

Abstract

Highlights: Lyophilised wafers for the local buccal delivery of econazole nitrate (ECN) were developed. Formulation contained low methoxy amidated pectin (LMAP) and carboxymethylcellulose (CMC). The drug was loaded as ternary cyclodextrin complex with citric acid (ECN/SBEβCD/CA). LMAP/CMC ratio was optimized by experimental design to obtain maximal mucoadhesivity. Optimized formulation released ECN at 5 mg/h rate, acting efficiently against selected Candida stains. 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 5 mg/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.