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Amidated pectin-based wafers for econazole buccal delivery: formulation optimization and antimicrobial efficacy
Paola Mura1, Natascia Mennini1, Ivan Kosalec2
1Department of Chemistry, School of Human Health Sciences, University of Florence, Via Schiff 6, Sesto Fiorentino I-50019, Florence, Italy.
Carbohydrate Polymers
|February 10, 2015
Summary
This study developed a novel oral wafer using pectin and carboxymethylcellulose to deliver econazole nitrate for treating oral candidiasis. The formulation demonstrated effective mucoadhesion, prolonged residence time, and controlled drug release, proving its therapeutic potential.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Mycology
Background:
- Oral candidiasis requires effective drug delivery systems for sustained treatment.
- Econazole nitrate (ECN) is an antifungal agent, but its oral delivery can be challenging.
- Developing mucoadhesive formulations can improve drug residence time and efficacy in the oral cavity.
Purpose of the Study:
- To formulate and optimize a lyophilized wafer for prolonged oral residence and controlled release of econazole nitrate.
- To evaluate the mucoadhesion strength, residence time, and in situ drug release of the developed buccal wafer.
- To assess the in vitro efficacy of the optimized formulation against Candida strains.
Main Methods:
- Lyophilized wafers were prepared using combinations of low-methoxy amidated pectin (LMAP) and carboxymethylcellulose (CMC).
- A ternary complex of ECN/sulphobutylether-ß-cyclodextrin/citric acid was incorporated into the wafer formulation.
- Experimental design was employed to optimize the formulation, followed by characterization of mucoadhesion, residence time, and drug release kinetics.
- In vitro antifungal activity was tested against selected Candida strains.
Main Results:
- The optimized wafer formulation exhibited significant mucoadhesion strength (28.37 ± 0.04 mg/cm(2)) and a residence time of 88.1 ± 0.1 min.
- The experimental values closely matched the predicted parameters, validating the formulation model.
- A constant in situ release of econazole nitrate at 5mg/h was achieved.
- The formulation demonstrated in vitro efficacy against tested Candida strains.
Conclusions:
- The developed lyophilized wafer formulation effectively delivers econazole nitrate for oral candidiasis therapy.
- The formulation's mucoadhesive properties and controlled release profile enhance its therapeutic potential.
- This novel delivery system offers a promising approach for managing oral fungal infections.
Keywords:
Buccal waferEconazole nitrateExperimental designLow methoxy amidated pectinMucoadhesionSulphobutylether-ß-cyclodextrinMore Related Videos
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