Membrane Interaction of Ibuprofen with Cholesterol-Containing Lipid Membranes
2020
Jan Kremkow | Meike Luck | Daniel Huster | Peter Müller | Holger A. Scheidt
Deciphering the membrane interaction of drug molecules is important for improving drug delivery, cellular uptake, and the understanding of side effects of a given drug molecule. For the anti-inflammatory drug ibuprofen, several studies reported contradictory results regarding the impact of ibuprofen on cholesterol-containing lipid membranes. Here, we investigated membrane localization and orientation as well as the influence of ibuprofen on membrane properties in POPC/cholesterol bilayers using solid-state NMR spectroscopy and other biophysical assays. The presence of ibuprofen disturbs the molecular order of phospholipids as shown by alterations of the <sup>2</sup>H and <sup>31</sup>P-NMR spectra of the lipids, but does not lead to an increased membrane permeability or changes of the phase state of the bilayer. <sup>1</sup>H MAS NOESY NMR results demonstrate that ibuprofen adopts a mean position in the upper chain/glycerol region of the POPC membrane, oriented with its polar carbonyl group towards the aqueous phase. This membrane position is only marginally altered in the presence of cholesterol. A previously reported result that ibuprofen is expelled from the membrane interface in cholesterol-containing DMPC bilayers could not be confirmed.
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