Fabrication of Modified Transport Fluconazole Transdermal Spray Containing Ethyl Cellulose and Eudragit® RS100 as Film Formers

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Springer US

RESUMO

The present investigation was undertaken to fabricate modified transport fluconazole transdermal spray using ethyl cellulose and Eudragit® RS100 as film-forming polymers. Eudragit® RS100 (X1) and ethyl cellulose (X2) were selected as independent variables in 32 full factorial design, whereas drug transport in first hour (Y1) and the time required for 50% drug transport (Y2) were selected as dependent variables. Eutectic blend of camphor and menthol was used as permeation enhancer cum solvent for film-forming polymers. The pH, viscosity, volume of solution delivered upon each actuation, spray angle, ex–in vivo physical evaluation and in vitro drug transport of the formulated products were evaluated. The optimized batch B16 containing 5.25% w/w ethyl cellulose and 10.6% w/w Eudragit® RS100 was formulated by overlapping the contour plots of Y1 and Y2. The pH, viscosity, volume of solution sprayed upon each actuation and spray angle of the batch B16 was 6.3, 52.9 cPs, 0.24 ml and 82.6° respectively. The film of optimized batch was flexible and dermal-adhesive. The responses Y1 and Y2 of batch B16 were 7.91 μg/ml and 347 min respectively. The kinetics of drug transport was best explained by the Korsmeyer and Peppas model. The eutectic mixture consisting of equal parts of camphor and menthol showed improved drug permeation through shed snake skin. Short-term stability study demonstrated insignificant changes in performance characteristics.

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