Formulation and in-vitro efficacy of antifungal mucoadhesive polymeric matrices for the delivery of miconazole nitrate

TEJADA, G.; PICCIRILLI, G.; SORTINO, M.; SALOMON, C.; LAMAS, M. C.; LEONARDI, D.

MATERIALS SCIENCE & ENGINEERING. C, BIOMIMETIC MATERIALS, SENSORS AND SYSTEMS

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2017 p. 140 - 150

0928-4931

Oral candidiasis is the most common opportunistic infection affecting patients with the human immunodeficiencyvirus. Miconazole buccal tablets or miconazole gel are approved for the treatment of oropharyngeal candidiasis.However, buccal films present more flexibility and also offer protection for the wounded mucosa,reducing pain. Due to their small size and thickness, buccal films may improve patients´ compliance, comparedto tablets. Additionally, they may increase the relatively short residence time on the mucosa of oral gels, whichare easily removed by saliva. Polymeric films loaded with miconazole nitrate were prepared by a casting/solventevaporation methodology using chitosan, carbopol, gelatin, gum arabic, and alginate to form the polymeric matrices.The morphology of films was investigated by scanning electron microscopy; interactions between polymerswere analyzed by infrared spectroscopy and drug crystallinity by differential thermal analysis and X-raydiffraction. Films were characterized in terms of thickness, folding endurance, tensile properties, swelling, adhesiveness,and drug release. Finally, the antifungal activity against cultures of the five most important fungal opportunisticpathogens belonging to Candida genus was investigated. The more appropriate formulations werethose based on chitosan-gelatin and chitosan-carbopol which showed good mechanical properties and adhesiveness,a relative low swelling index, improved drug release, and showed better in vitro activity against Candida culturesthan miconazole nitrate raw material. Thus, it will be possible to produce a new pharmaceutical form basedon polymeric films containing chitosan and miconazole nitrate, which could be loaded with low drug concentrationproducing the same therapeutic effect against Candida cultures.