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Losartan Interactions with 2-Hydroxypropyl-β-CD
Authors:Vasiliki Palli  Georgios Leonis  Nikoletta Zoupanou  Nikitas Georgiou  Maria Chountoulesi  Nikolaos Naziris  Demeter Tzeli  Costas Demetzos  Georgia Valsami  Konstantinos D. Marousis  Georgios A. Spyroulias  Thomas Mavromoustakos
Abstract:Losartan potassium salt (LSR) is a well-known antihypertensive drug with proven beneficial effects on human health. Its formulation with the non-toxic 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD) could improve its pharmacological profile. Thus, its molecular interactions are studied using a combination of Differential Scanning Calorimetry (DSC), Nuclear Magnetic Resonance (NMR) and Molecular Dynamics (MD). First, its complexation is shown through Differential Scanning Calorimetry as lyophilization provided distinct thermal properties in comparison to the mixture. The complexation is further proved by utilizing the chemical shift changes in the complexation and T1 values. Furthermore, the reversible favorable complexation was shown by MD calculations. Such physical chemical properties provide evidence that this formulation must be further explored through biological experiments.
Keywords:losartan, hydroxypropyl-β  -cyclodextrin, molecular interactions, differential scanning calorimetry, nuclear magnetic resonance, molecular dynamics
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