Amphiphilic drug interactions with model cellular membranes are influenced by lipid chain-melting temperature

Duncan Casey; Kalypso Charalambous; Antony Gee; Robert V. Law; Oscar Ces

doi:10.1098/rsif.2013.1062

Amphiphilic drug interactions with model cellular membranes are influenced by lipid chain-melting temperature

Duncan Casey, Kalypso Charalambous, Antony Gee, Robert V. Law, Oscar Ces^*

^*Corresponding author for this work

School of Biochemistry

Research output: Contribution to journal › Article (Academic Journal) › peer-review

23 Citations (Scopus)

284 Downloads (Pure)

Abstract

Small-molecule amphiphilic species such as many drug molecules frequently exhibit low-to-negligible aqueous solubility, and generally have no identified transport proteins assisting their distribution, yet are able to rapidly penetrate significant distances into patient tissue and even cross the blood-brain barrier. Previous work has identified a mechanism of translocation driven by acid-catalysed lipid hydrolysis of biological membranes, a process which is catalysed by the presence of cationic amphiphilic drug molecules. In this study, the interactions of raclopride, a model amphiphilic drug, were investigated with mixtures of biologically relevant lipids across a range of compositions, revealing the influence of the chain-melting temperature of the lipids upon the rate of acyl hydrolysis.

Original language	English
Article number	20131062
Number of pages	7
Journal	Journal of the Royal Society Interface
Volume	11
Issue number	94
Early online date	12 Mar 2014
DOIs	https://doi.org/10.1098/rsif.2013.1062
Publication status	Published - 6 May 2014

Keywords

Drug transport
High-performance liquid chromatography
Lipid hydrolysis
Membrane biophysics

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10.1098/rsif.2013.1062

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AU - Ces, Oscar

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Amphiphilic drug interactions with model cellular membranes are influenced by lipid chain-melting temperature

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Keywords

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