TY - JOUR
TI - Exploring the interactions of irbesartan and irbesartan–2-hydroxypropyl-β-cyclodextrin complex with model membranes
AU - 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
JO - Biochimica et Biophysica Acta (BBA)
PY - 2017
VL - 1859
TODO - -
SP - 1089-1098
PB - Elsevier
SN - 0006-3002
TODO - null
TODO - Irbesartan; DPPC; HP-β-CD; Molecular Dynamics; Small Angle Xray Scattering
TODO - 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.
ER -