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Firocoxib nanocrystals: Preparation, characterization, and pharmacokinetics in beagle dogs

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Autor(es):
Macedo, Luiza de Oliveira ; da Silva, Rosana Pereira ; de Jesus, Daniel Felipe Freitas ; Bragard, Andre Sampaio ; de Araujo, Gabriel Lima Barros ; Ferraz, Humberto Gomes ; Ishida, Kelly ; Bou-Chacra, Nadia Araci
Número total de Autores: 8
Tipo de documento: Artigo Científico
Fonte: International Journal of Pharmaceutics; v. 679, p. 15-pg., 2025-06-30.
Resumo

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 C-max 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. (AU)

Processo FAPESP: 21/12869-8 - Nanocristais de firocoxibe para o manejo da osteoartrite veterinária: desenvolvimento, caracterização físico-química e avaliação da segurança in vitro
Beneficiário:Isabela Fernandes de Oliveira
Modalidade de apoio: Auxílio à Pesquisa - Pesquisa Inovativa em Pequenas Empresas - PIPE