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Article

Membrane Interaction of Ibuprofen with Cholesterol-Containing Lipid Membranes

1
Institute for Medical Physics and Biophysics, Leipzig University, Härtelstr. 16-18, D-04107 Leipzig, Germany
2
Department of Biology, Humboldt University Berlin, Invalidenstr. 42, D-10115 Berlin, Germany
*
Author to whom correspondence should be addressed.
Both Authors contributed equally.
Biomolecules 2020, 10(10), 1384; https://doi.org/10.3390/biom10101384
Received: 11 August 2020 / Revised: 25 September 2020 / Accepted: 26 September 2020 / Published: 28 September 2020
(This article belongs to the Section Molecular Structure and Dynamics)
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 2H and 31P-NMR spectra of the lipids, but does not lead to an increased membrane permeability or changes of the phase state of the bilayer. 1H 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. View Full-Text
Keywords: ibuprofen; cholesterol; membrane interaction; NMR; fluorescence; membrane properties ibuprofen; cholesterol; membrane interaction; NMR; fluorescence; membrane properties
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MDPI and ACS Style

Kremkow, J.; Luck, M.; Huster, D.; Müller, P.; Scheidt, H.A. Membrane Interaction of Ibuprofen with Cholesterol-Containing Lipid Membranes. Biomolecules 2020, 10, 1384. https://doi.org/10.3390/biom10101384

AMA Style

Kremkow J, Luck M, Huster D, Müller P, Scheidt HA. Membrane Interaction of Ibuprofen with Cholesterol-Containing Lipid Membranes. Biomolecules. 2020; 10(10):1384. https://doi.org/10.3390/biom10101384

Chicago/Turabian Style

Kremkow, Jan, Meike Luck, Daniel Huster, Peter Müller, and Holger A. Scheidt 2020. "Membrane Interaction of Ibuprofen with Cholesterol-Containing Lipid Membranes" Biomolecules 10, no. 10: 1384. https://doi.org/10.3390/biom10101384

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