Losartan Interactions with 2-Hydroxypropyl-β-CD

Author:

Palli Vasiliki,Leonis GeorgiosORCID,Zoupanou Nikoletta,Georgiou NikitasORCID,Chountoulesi Maria,Naziris NikolaosORCID,Tzeli DemeterORCID,Demetzos Costas,Valsami GeorgiaORCID,Marousis Konstantinos D.,Spyroulias Georgios A.ORCID,Mavromoustakos ThomasORCID

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.

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

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