Physicochemical characterization and evaluation of polarity influence in eutectic systems applied to drug solubility

LORENZETTI, ANABELA; SAMUELSEN LUCEA, CLAUS; FEAÑO, VERÓNICA; SILVA, MARÍA FERNANDA; GOMEZ, FEDERICO; DOMINI, CLAUDIA

JOURNAL OF MOLECULAR LIQUIDS

ELSEVIER SCIENCE BV

Año: 2024 vol. 411

0167-7322

In the process of discovery and development of APIs (Active Pharmaceutical Ingredients), the rate of solubility oraqueous dissolution plays a very important role from the first evaluations of the candidates to the development offinal marketable products. Since only the solubilized form of an active ingredient is capable of being transportedand exerting its therapeutic effect across biological membranes, it is of utmost importance to control its solubility. However, the number of APIs under development with low water solubility has notoriously grown inrecent years. Their pharmaceutical use will face problems such as insufficient bioavailability, late onset of action,and the need for large dosages.The present study aims to evaluate the behavior of ciprofloxacin and norfloxacin (fluoroquinolones), as modelAPIs for their different solubilities, in aqueous and non-aqueous natural deep eutectic solvents (NADES). Themain objective is to improve the solubility of both drugs in pharmaceutical studies and analytical applications. Inorder to do so, two sets of eutectic solvents were selected, each composed with a polar solvent, an intermediateone, and a nonpolar solvent, as well. Very promising results were obtained in NADES of polar and intermediatepolarity, for both drugs. In addition, the physicochemical characterization of such solvents was carried out tobetter understand the aforementioned results