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Rational design of natural deep eutectic solvents contributes to desirable shift of ciprofloxacin in Biopharmaceutics classification system
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Resumo(s)
Considerable efforts are being directed toward developing novel drug formulations to address challenges encountered in the pharmaceutical industry, notably concerning drug solubility and permeability. In this context, environmentally friendly approaches are being explored, including the utilization of natural deep eutectic solvents (NADES). These solvents exhibit great versatility, since they could serve as a dissolution medium for active pharmaceutical ingredients (APIs), facilitate drug synthesis, and function as drug carriers or delivery systems. The vast array of possible combinations inherent in NADES, often referred to as designer solvents, emphasizes their potential. Consequently, the selection of appropriate NADES for enhancing the formulation of the antibiotic ciprofloxacin (CIP) was conducted via in silico modelling using COSMOtherm software. Evaluation of CIP solubility in over 70 NADES lead to the preparation of five candidates, which were then experimentally assessed for CIP solubility. Among these, the hydrophobic NADES thymol:octanoic acid (Ty:C8) (1:3) demonstrated the highest solubility of CIP. Subsequent investigations included assessment of permeability and stability over a 90-day period, whereas antimicrobial activity and cytocompatibility test were focused on the best variant Ty:C8. The dissolution of CIP in NADES Ty:C8 notably enhanced its solubility, while maintaining its antimicrobial activity and stability. However, no improvement in permeability was observed, what in overall contributes to the BSC reclassification from class 4 to class 3.
Descrição
Funding Information: This work was developed through the Croatian Science Foundation Project (IP-2019-04-7712) and supported by the EU COST Action (CA18224 – Greenering) through Short Term Scientific Mission of M. Panić. Publisher Copyright: © 2024 Elsevier B.V.
Palavras-chave
Ciprofloxacin COSMOtherm Natural deep eutectic solvents Permeability Solubility Electronic, Optical and Magnetic Materials Atomic and Molecular Physics, and Optics Condensed Matter Physics Spectroscopy Physical and Theoretical Chemistry Materials Chemistry