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19F Solid-State NMR and Vibrational Raman Characterization of Corticosteroid Drug-Lipid Membrane Interactions

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19F Solid-State NMR and Vibrational Raman Characterization of Corticosteroid Drug-Lipid Membrane Interactions. / Mapley, Bethany; Townsend, David; Griffin, John; Ashton, Lorna; Middleton, David.

In: ChemPlusChem, Vol. 86, No. 11, 15.11.2021, p. 1517-1523.

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@article{5444e7a482ba41b495d265f96794b349,
title = "19F Solid-State NMR and Vibrational Raman Characterization of Corticosteroid Drug-Lipid Membrane Interactions",
abstract = "Drug interactions with phospholipid bilayers underpin their behaviour in cell membranes and in liposomal delivery formulations. Liposomal drug delivery in ocular medicine can overcome the physical barriers of the eye and better enable the active molecule to reach its target. Here, Raman and 19F solid-state NMR spectroscopy are used to characterise the interactions of two ocular corticosteroid drugs, difluprednate (DFP) and fluorometholone (FML), with multilamellar vesicles of phosphatidylcholine (PC). 31P NMR confirms that the lipid bilayer tolerates a high drug concentration (a drug: lipid molar ratio of 1 : 10). The 19F NMR spectra of the drugs in lipid bilayers reveal that FML and DFP have different average orientations within the lipid bilayer. Raman spectra of dried lipid films reveal that PC separates from DFP but not from FML, the less lipophilic of the two drugs. This combined approach will assist the design of, and inform the development of, improved liposomal preparations.",
keywords = "drug delivery, lipid bilayers, phospholipid vesicles, Raman spectroscopy, solid-state NMR",
author = "Bethany Mapley and David Townsend and John Griffin and Lorna Ashton and David Middleton",
year = "2021",
month = nov,
day = "15",
doi = "10.1002/cplu.202100385R2",
language = "English",
volume = "86",
pages = "1517--1523",
journal = "ChemPlusChem",
issn = "2192-6506",
publisher = "Wiley-VCH Verlag",
number = "11",

}

RIS

TY - JOUR

T1 - 19F Solid-State NMR and Vibrational Raman Characterization of Corticosteroid Drug-Lipid Membrane Interactions

AU - Mapley, Bethany

AU - Townsend, David

AU - Griffin, John

AU - Ashton, Lorna

AU - Middleton, David

PY - 2021/11/15

Y1 - 2021/11/15

N2 - Drug interactions with phospholipid bilayers underpin their behaviour in cell membranes and in liposomal delivery formulations. Liposomal drug delivery in ocular medicine can overcome the physical barriers of the eye and better enable the active molecule to reach its target. Here, Raman and 19F solid-state NMR spectroscopy are used to characterise the interactions of two ocular corticosteroid drugs, difluprednate (DFP) and fluorometholone (FML), with multilamellar vesicles of phosphatidylcholine (PC). 31P NMR confirms that the lipid bilayer tolerates a high drug concentration (a drug: lipid molar ratio of 1 : 10). The 19F NMR spectra of the drugs in lipid bilayers reveal that FML and DFP have different average orientations within the lipid bilayer. Raman spectra of dried lipid films reveal that PC separates from DFP but not from FML, the less lipophilic of the two drugs. This combined approach will assist the design of, and inform the development of, improved liposomal preparations.

AB - Drug interactions with phospholipid bilayers underpin their behaviour in cell membranes and in liposomal delivery formulations. Liposomal drug delivery in ocular medicine can overcome the physical barriers of the eye and better enable the active molecule to reach its target. Here, Raman and 19F solid-state NMR spectroscopy are used to characterise the interactions of two ocular corticosteroid drugs, difluprednate (DFP) and fluorometholone (FML), with multilamellar vesicles of phosphatidylcholine (PC). 31P NMR confirms that the lipid bilayer tolerates a high drug concentration (a drug: lipid molar ratio of 1 : 10). The 19F NMR spectra of the drugs in lipid bilayers reveal that FML and DFP have different average orientations within the lipid bilayer. Raman spectra of dried lipid films reveal that PC separates from DFP but not from FML, the less lipophilic of the two drugs. This combined approach will assist the design of, and inform the development of, improved liposomal preparations.

KW - drug delivery

KW - lipid bilayers

KW - phospholipid vesicles

KW - Raman spectroscopy

KW - solid-state NMR

U2 - 10.1002/cplu.202100385R2

DO - 10.1002/cplu.202100385R2

M3 - Journal article

VL - 86

SP - 1517

EP - 1523

JO - ChemPlusChem

JF - ChemPlusChem

SN - 2192-6506

IS - 11

ER -