In vitro evaluation of mucoadhesive buccal films loaded with miconazole nitrate

TEJADA, G.; BARRERA M. G.; PICCIRILLI, G.N.; FRATTINI, A.; SALOMON C.J.; LAMAS, M. C.; BIASOLI, M.S.; LUQUE, A.G.; LEONARDI, D.

Cordoba, Argentina

Congreso; III Reunión Internacional de Ciencias Farmacéuticas RICIFA; 2014

Buccal mucoadhesive films, releasing drugs in the oral cavity provide alternatives to the traditional dosage forms for treatment of oral candidiasis. The aim of this work was the development and full characterization of polymeric films loaded with miconazole nitrate (MN) as model drug. Three different formulations containing MN, polyethylene glycol 400 (PEG 400), as plasticizer, and chitosan (CH) and pectin (PC) as film-forming polymers, were prepared by the casting method. Films were characterized in terms of thickness, mechanical strengths, and swelling capacity. Adhesion of films was assayed using pig buccal mucosa. Interactions between polymers were analyzed by Fourier-transform infrared spectroscopy, thermal gravimetric analysis and differential scanning calorimetry. Morphology of the matrices was investigated by scanning electron microscopy. MN release and in vitro microbiological effectiveness against Candida parapsilosis were evaluated. CH was solubilized in aqueous lactic acid solution (2% v/v) and stirred overnight. PC solutions were prepared by dissolution in water. CH solutions were dripped to the PC solutions, then MN solubilized in PEG 400 was added and the mixture was stirred at 200 rpm during 2 h. The solutions were cast on petri dishes and dried in an oven at 35 °C. The compositions of matrixes were combinations between CH and PC, all loaded with MN. Thickness the films ranged from 0.6818 to 0.7389 mm and its weights from 406.9 to 653.7 mg. Adhesion (0.20 to 0.30 N) and mechanical properties (tensile strength 0.5 to 0.95 N/mm and elongation 3.39 to 10.88 mm) were in adequate range. The swelling percent of the films after 6 h ranged from 68.8% to 197.5%. The antifungal in vitro activity was confirmed by the generation of inhibition halos (31 to 52 mm) in candida culture dishes. Thus, CH-PC buccal films containing MN could be a convenient approach for the treatment of oral candidiasis.