Films based on chitosan/carbopol polyelectrolyte complex containing econazole nitrate for the treatment of cutaneous candidiasis

MARINELICH, D.M.; FRATTINI, A.; LUQUE, A.G.; BIASOLI, M.S.; OLIVIERI, A.C.; LEONARDI, D.

Cordoba, Argentina

Congreso; I Reunión internacional de Ciencias Farmacéuticas (Ricifa).; 2010

Universidades Nacionales de Córdoba y Rosario

One of the aims of dermal delivery is to localize a drug within the skin in order to enhance a local effect. In the case of dermato-pharmacotherapy for the treatment of skin inflammation, acne and skin fungal infections, the dermal delivery of active ingredients is desirable. The conventional dosage forms for the treatment of skin micosis are creams, ointments, solutions and powders (1 %). The affected zone must be covered with the dosage form three times daily, generating an erratic drug concentration in the target site. Bioadhesive films based on polyelectrolyte complexes are a good alternative to conventional dosage forms, because they allow to apply an exact drug concentration on the target site and to control the release of the drug. This could be reflected in a reduction of the number of applications. The polyelectrolyte complexes are obtained by electrostatic interactions between two polymers with opposite charge, without the use of organic solvents. The aim of this work was to develop bioadhesive films employing chitosan and carbopol 940®, for the controll of release of econazole nitrate at different concentrations.Chitosan (3 % w/v) was dissolved in lactic acid (2 % v/v) and carbopol 940® (1 % w/v) in water. 20 ml of each solution were mixed for 5 minutes and the pH was fixed at either 2 or 5. Finally, 1 ml of glycerol (as plasticizing) and econazole nitrate at different concentrations (0; 0.01; 0.05; 0.10; 0.25; 0.5 y 1% w/v) were added. Film forming solutions were mechanically stirred at 800 rpm for 2 hs, cast on Petri-dishes and dried at 35 ºC for 48 hs. Dried films were conditioned in a desiccator containing a saturated solution of NaCl at 25 ºC (75% RH).The interactions between the polymers were investigated by infrared spectroscopy (IR) and differential thermal analysis and thermogravimetry (DTA-TG). The film surfaces were studied by scaning electron microscopy (SEM) and atomic force microscopy (AFM). The in vitro activity of the complex was evaluated by the difussion method in an agar Müeller Hinton medium, using Candida krusei ATCC 6258 as control. Plates were incubated at 37 ºC and the activity of the the films was evaluated by transfers until 24 hs (measuring the inhibition hales).