beta-cyclodextrin complexation as an approach to enhance the biopharmaceutical properties of Norfloxacin B Hydrate

• Autor(a) principal: Soledad Bueno, Maria
• Data de Publicação: 2019
• Outros Autores: Chierentin, Lucas [UNESP], Bongioanni, Agustina, Nunes Salgado, Herida Regina [UNESP], Raquel Longhi, Marcela, Garnero, Claudia
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Institucional da UNESP
• Texto Completo: http://dx.doi.org/10.1016/j.carres.2019.107818; http://hdl.handle.net/11449/197513
• topic: Norfloxacin; Polymorphism; Bioassay; Cyclodextrin complexation; Solubility

Binary systems of Norfloxacin B Hydrate with beta-CD were explored by reliable biopharmaceutical studies as potential candidates for the preparation of drug delivery systems. Initially, studies of antimicrobial activity and solubility of the different polymorphic forms of Norfloxacin provided evidence to select Norfloxacin B Hydrate as the optimal solid form of Norfloxacin. Solid binary systems were preparing by kneading, freeze-drying, and physical mixture methods. The influence on the solubility, dissolution rate and chemical stability of Norfloxacin B Hydrate was investigated. These studies showed an increment of solubility and dissolution rate in physiological simulated fluids. However, the solid systems were moderated hygroscopically under accelerated storage conditions, which produces a destabilizing effect that accelerated the chemical reactivity of the drug in such conditions. Therefore, special cares must be considered in the manufacturing process and the packaging selection. Moreover, the experimental results proved that freeze-drying was not an appropriate method for the preparation. In conclusion, the Norfloxacin oral bioavailability can be improved with this binary systems, that could be applied in the production of an alternative pharmaceutical formulation of the drug.