Studies of the Formation and Stability of Ezetimibe-Cyclodextrin Inclusion Complexes

Int J Mol Sci. 2021 Dec 31;23(1):455. doi: 10.3390/ijms23010455.

Abstract

In the presented studies, the interactions between ezetimibe (EZE) and selected cyclodextrins were investigated. α-Cyclodextrin (αCD), β-cyclodextrin (βCD) and its modified derivatives, hydroxypropyl-β-cyclodextrin (HPβCD) and sulfobutylether-β-cyclodextrin (SBEβCD), were selected for the research. Measurements were carried out using calorimetric and spectroscopic methods. Additionally, the Hirshfeld surface and biochemical analysis were achieved. As a result of the study, the inclusion complexes with 1:1 stoichiometry were obtained. The most stable are the complexes of β-cyclodextrin and its derivatives. The comparison of βCD with its derivatives shows that the modifications have an affect on the formation of more durable and stable complexes.

Keywords: FT-IR; HNMR; cyclodextrins; differential scanning calorimetry; formation constant; isothermal titration calorimetry; mitochondrial permeability transition.

MeSH terms

  • Chemistry, Pharmaceutical / methods
  • Cyclodextrins / chemistry*
  • Ezetimibe / chemistry*
  • Thermodynamics

Substances

  • Cyclodextrins
  • Ezetimibe