Isoniazid‐loaded orodispersible strips: Methodical design, optimization and in vitro‐in silico characterization

Graphical abstract Figure. No caption available. ABSTRACT Drug treatment remains the most effective global approach to managing and preventing tuberculosis. This work focuses on formulating and evaluating an optimized polyvinyl alcohol‐polyethylene glycol based orodispersible strip containing isoniazid, a first‐line anti‐tubercular agent. A solvent casting method guided through a Taguchi experimental design was employed in the fabrication, optimization and characterization of the orodispersible strip. The optimized strip was physically amalgamated with a monolayer, uniformly distributed surface geometry. It was 159.2 ± 3.0 &mgr;m thick, weighed 36.9 ± 0.3 mg, had an isoniazid load of 99.5 ± 0.8%w/w, disintegration and dissolution times of 17.6 ± 0.9 s and 5.5 ± 0.1 min respectively. In vitro crystallinity, thermal measurements and in silico thermodynamic predictions confirmed the strip's intrinsic miscibility, thermodynamic stability and amorphous nature. A Korsmeyer‐Peppas (r = 0.99; n > 1 = 1.07) fitted kinetics typified by an initial burst release of 49.4 ± 1.9% at 4 min and a total of 99.8 ± 3.3% at 30 min was noted. Ex vivo isoniazid permeation through porcine buccal mucosa was bi‐phasic and characterized by a 50.4 ± 3.8% surge and 95.6 ± 2.9% at 5 and 120 min respectively. The strip was physicomechanically robust, environmentally stable and non‐cytotoxic.

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