The aims of our investigation were to develop and optimize ciclopirox (CPX) nail lacquer using nonbiodegradable Eudragit RLPO (E-RLPO) as a film former and to assess its penetration efficiency across the human nail plate. Preliminary trials such as hydration enhancement factor (HEF), a retained drug in the nail plate, and SEM were studied to select the optimized permeation enhancer to be incorporated in the optimized lacquer formulation. A 3 full factorial design was built up to study the effect of three different factors, concentration of E-RLPO (10, 20, and 30%), Tween 80 (0.25, 0.5, and 1%), and triacetin (0, 10, and 30% of polymer weight). The studied responses were the drying time, water resistance, viscosity, and drug release up to 4 h. An ex vivo permeation study for the optimized formulations was carried out. The preliminary study aided the selection of 5% papain (endopeptidase enzyme) as a penetration enhancer; it showed the highest HEF of 15.27%, the highest amount of drug retained in the nail plate (886.2 μg/g). An ex vivo permeation study guided the selection of F4B (flux value of 3.79 μg/cm/h) as optimized formulation. The optimized lacquer formula showed threefold increases in the permeation than the marketed CPX lacquer (Batrafen®). Confocal laser scanning microscopy revealed the higher intensity of the Rhodamine B dye across the nail plate in the case of the formula containing papain than the marketed formula without papain. Conclusively, an efficient and stable nail lacquer was developed for potential transungual delivery of CPX to target the drug to the nail bed and ensure efficiency against onychomycosis.
Objective: The aim of this work is to investigate the influence of different casting solvents on the physicochemical properties of cetylpyridinium chloride (CPC) chitosan mucoadhesive buccal films.Methods: Screening formulations were prepared by casting solvent technique using organic acids; 1% acetic acid (AA), 1% lactic acid (LA) and inorganic acid; 0.1N HCl (FS1-FS3). Then, 2P 1 P X3P 1 P factorial design study was done using 2 factors; solvent type (AA, LA, Mixture of 0.1N HCl and LA) and solvent concentration (AA and LA; 1%, 2% and mixture of 0.1N HCl: 1% LA; 2:1, 1:2). Films were evaluated for their physicochemical properties through, mechanical properties, mucoadhesion, in vitro release of CPC and antimicrobial activity.
Results:The studied factors showed a significant effect on both mucoadhesion and tensile strength. Film casted from 0.1 N HCl was brittle and did not show any elasticity, so it was used in further studies mixed with LA to improve physicochemical properties of the prepared films. Films casted from LA showed swelling for an initial period of 15 min then no more swelling occurred while swelling of those casted from AA occurred throughout approximately 2 h. A film containing 2:1 HCl: LA (F5) dissolved in both media while 1:2 HCl: LA (F6) showed swelling properties. This was reflected on the in vitro release of CPC in which F5 gave higher % released (DER 300 min R54.37%) than the other formulations.
Conclusion:Casting solvent was proved to have a significant effect on the physicochemical properties of chitosan CPC mucoadhesive films.
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