Amphiphilic drug interactions with model cellular membranes are influenced by lipid chain-melting temperature.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 24621813.
- Also identified by DOI 10.1098/rsif.2013.1062 and PMC identifier 3973356.
- Licence recorded as CC BY.
- The licence permits redistribution, so the abstract is shown in full and the full text is available from the publisher.
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.
Medical subject headings
- Membrane Lipids
- Membranes, Artificial
- Models, Chemical
- Raclopride