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Abstract
The goal was to develop an optimized transdermal finasteride (FNS) film loaded with
drug microplates (MIC), utilizing two-step optimization, to decrease the dosing schedule
and inconsistency in gastrointestinal absorption. First; 3-level factorial design
was implemented to prepare optimized FNS-MIC of minimum particle size. Second; Box-Behnken
design matrix was used to develop optimized transdermal FNS-MIC film. Interaction
among MIC components was studied using physicochemical characterization tools. Film
components namely; hydroxypropyl methyl cellulose (X1), dimethyl sulfoxide (X2) and
propylene glycol (X3) were optimized for their effects on the film thickness (Y1)
and elongation percent (Y2), and for FNS steady state flux (Y3), permeability coefficient
(Y4), and diffusion coefficient (Y5) following ex-vivo permeation through the rat
skin. Morphological study of the optimized MIC and transdermal film was also investigated.
Results revealed that stabilizer concentration and anti-solvent percent were significantly
affecting MIC formulation. Optimized FNS-MIC of particle size 0.93μm was successfully
prepared in which there was no interaction observed among their components. An enhancement
in the aqueous solubility of FNS-MIC by more than 23% was achieved. All the studied
variables, most of their interaction and quadratic effects were significantly affecting
the studied variables (Y1-Y5). Morphological observation illustrated non-spherical,
short rods, flakes like small plates that were homogeneously distributed in the optimized
transdermal film. Ex-vivo study showed enhanced FNS permeation from film loaded MIC
when compared to that contains pure drug. So, MIC is a successful technique to enhance
aqueous solubility and skin permeation of poor water soluble drug especially when
loaded into transdermal films.