Τμήμα Χημείας

Exploring the interactions of irbesartan and irbesartan–2-hydroxypropyl-β-cyclodextrin complex with model membranes

Αγγλικά

The interactions of irbesartan (IRB) and irbesartan–2-hydroxypropyl-βcyclodextrin (HP-β-CD) complex with Dipalmitoyl Phosphatidylcholine (DPPC)
bilayers have been explored utilizing an array of biophysical techniques ranging
from Differential Scanning Calorimetry (DSC), Small angle X-ray Scattering
(SAXS), ESI Mass-Spectrometry (ESI-MS) and solid state Nuclear Magnetic
Resonance (ssNMR). Molecular Dynamics (MD) calculations have been also
conducted to complement the experimental results. Irbesartan was found to be
embedded in the lipid membrane core and to affect the phase transition properties
of the DPPC bilayers. SAXS studies revealed that irbesartan alone does not
display perfect solvation since some coexisting irbesartan crystallites are present.
In its complexed form IRB gets fully solvated in the membranes showing that
encapsulation of IRB in HP-β-CD may have beneficial effects in the ADME
properties of this drug. MD experiments revealed the topological and orientational
integration of irbesartan into the phospholipid bilayer being placed at about 1 nm
from the membrane centre.

2017

Α. S. Liossi , D. Ntountaniotis, T.F. Kellici, M.V. Chatziathanasiadou, G. Megariotis, M. Mania, J. Becker-Baldus, M. Kriechbaum, A. Krajnc, E. Christodoulou, C. Glaubitz , M. Rappolt, H. Amenitsch, Gregor Mali, D.N. Theodorou, G. Valsami, M. Pitsikalis, H. Iatrou, A. Tzakos, T. Mavromoustakos

Biochimica et Biophysica Acta (BBA)

Elsevier

1859

-

1089-1098

Irbesartan; DPPC; HP-β-CD; Molecular Dynamics; Small Angle Xray Scattering

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