Pharmaceutical Nanococrystals of Norfloxacin: Synthesis and Characterization

• Grant number: 25/24291-1
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: December 01, 2025
• End date: November 30, 2026
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Analytical Chemistry
• Principal Investigator: Flávio Junior Caires
• Grantee: Manuela Germino
• Host Institution: Faculdade de Ciências (FC). Universidade Estadual Paulista (UNESP). Campus de Bauru. Bauru , SP, Brazil
• Associated research grant: 25/13146-0 - Pharmaceutical nanococrystals of norfloxacin: synthesis and characterization, AP.R

Abstract

Norfloxacin (NOR) is a broad-spectrum antibiotic that belongs to the second generation of the fluoroquinolone family, and is used to treat urinary tract infections, sexually transmitted diseases, prostatitis, and skin and soft tissue infections. It is an Active Pharmaceutical Ingredient (API) belonging to class IV of the Biopharmaceutical Classification System (BCS), with low aqueous solubility and low permeability. Several strategies have been developed to improve the physicochemical properties of APIs, such as the cocrystallization technique, which involves the intermolecular interaction between the drug and a coformer, generating a crystalline multicomponent solid that does not compromise the therapeutic action of the API. In addition to cocrystallization, nanotechnology is also applicable to improve the solubility of APIs, but the combination of both strategies is in the early stages of development. NOR will be cocrystallized with nicotinic acid (NCA), a B complex vitamin (B3) that has lipid-modifying properties. The NOR:NCA cocrystal has demonstrated pharmaceutical efficacy in terms of solubility, facilitating its use as a model system in the production of nanococrystals. The synthesis of the cocrystals, as well as the nanococrystals, will be performed by the mechanochemical method, in the absence or presence of small amounts of solvent, and the systems will be characterized by thermoanalytical, diffractometric and spectroscopic techniques. The size and morphology of the nanoparticles will be evaluated by scanning electron microscopy (SEM) and dynamic light scattering (DLS). The solubility of the system will be evaluated by the shake-flask method, following validated analytical methodology. (AU)