This study aimed to develop drug nanocrystals to enhance the aqueous solubility of firocoxib, an anti-inflammatory drug used in the treatment of pain in the veterinary field. Different non-ionic stabilizers were evaluated to obtain firocoxib nanocrystals with reduced particle size, increased saturation solubility, and adequate storage stability. Optimization using the Box-Behnken design resulted in nanocrystals with a particle size of < 200 nm. In vitro dissolution testing demonstrated a 1.5-fold increase in drug dissolution compared to the pure drug. Safety assessment in Galleria mellonella L. larvae revealed any acute toxicity below a dosage of 50 times. In the pharmacokinetic study in beagle dogs, the nanocrystals improved Cmax in 2x compared to commercial product. Physicochemical stability was maintained over 12 months, with reduced variability in particle size and a PdI < 0.3. Additionally, an exploratory scale-up study successfully produced 3000 g of firocoxib nanocrystals with particle size < 400 nm. These findings suggest that firocoxib nanocrystals have the potential to enhance drug absorption and enabling faster symptom relief from inflammation and pain in dogs.
Keywords: Anti-inflammatory; Drug nanocrystal; Firocoxib; Oral absorption; Pharmacokinetics.
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