A Natural Deep Eutectic Solvent Formulated to Stabilize β-Lactam Antibiotics

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dc.contributor.authorOlivares, Belen
dc.contributor.authorMartínez, Fabián
dc.contributor.authorRivas, Lina
dc.contributor.authorCalderon, Cristian
dc.contributor.authorMunita, José
dc.contributor.authorCampodónico, Paola
dc.date.accessioned2021-08-27T15:25:46Z
dc.date.available2021-08-27T15:25:46Z
dc.date.issued2018
dc.description.abstractβ-lactam antibiotics, such as penicillin share a very unstable chemical structure. In water-based solutions, such as those used for clinical applications, the β-lactam ring is readily opened due to a nucleophilic or electrophilic attack, leading to the loss of antimicrobial activity. Since the achievement and maintenance of optimum therapeutic levels of β-lactam antibiotics is critical for the resolution of many infectious clinical situations, and to avoid antibiotic resistance generation, the design of new non-aqueous dosage forms is urgent. Recently, natural deep eutectic solvents (NADES) have emerged as alternative non-toxic and non-aqueous solvents for different biomedical applications. In this work, we formulated and characterized a NADES composed by betaine and urea (BU). Using this solvent, we evaluated the stability of clavulanic acid (CLV) and imipenem (IMP) and characterized their antimicrobial activities calculating the minimal inhibitory concentration. Characterization of BU solvent by infrared spectroscopy (IR) and nuclear magnetic resonance spectroscopy (NMR) indicated that the obtained solvent has a microstructure mainly based on hydrogen bonding interactions and water addition strongly affects its dynamic. The stability of β-lactam antibiotic IMP and CLV using this solvent was increased by 7 fold and 2.5 fold respectively compared to water when analysed seven days after being dissolved. Microbiological assays showed that antibacterial activity at day seven was significantly decreased for both CLV and IMP when dissolved in water, while no change in their antibacterial properties was observed when antibiotics were dissolved in BU. The increased stability of IMP and CLV in BU may be related to the inert behaviour of the solvent and the higher dynamic restriction that helps antibiotics to maintain a more stable conformation. These data suggest the potential use of BU as a solvent to prevent degradation of β-lactam antibiotics.es
dc.identifier.citationScientific Reports volume 8, Article number: 14900 (2018)es
dc.identifier.urihttps://doi.org/10.1038/s41598-018-33148-wes
dc.identifier.urihttp://hdl.handle.net/11447/4499
dc.language.isoenes
dc.subjectNatural Deep Eutectic Solvents (NADES)es
dc.subjectBetainees
dc.subjectClavulanic Acides
dc.subjectNuclear Magnetic Resonance Spectroscopyes
dc.subjectMcFarland Inoculumes
dc.titleA Natural Deep Eutectic Solvent Formulated to Stabilize β-Lactam Antibioticses
dc.typeArticlees

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