Rapid colorimetric screening of drug interaction and penetration through lipid barriers

Pharmaceutical Research
Marina KatzRaz Jelinek

Abstract

The aims of this study are to develop a rapid colorimetric assay for evaluating membrane interactions and penetration through lipid barriers and to create a platform, amenable to high-throughput screening formats, for predicting the extent of penetration of pharmaceutical compounds through lipid layers. The colorimetric platform comprises vesicles of phospholipids and the chromatic lipid-mimetic polymer polydiacetylene. The polymer undergoes visible, concentration-dependent blue-red transformations induced through interactions of the vesicles with the molecules examined. We observe rapid colorimetric transitions induced by addition of pharmaceutical compounds to the chromatic vesicle solutions. We find that the concentration ranges for which the color transitions are induced in the lipid/polymer vesicles are correlated with the degree of lipid interactions and bilayer penetration of the tested compounds. The colorimetric platform could distinguish between three primary types of membrane-permeation profiles: bilayer-surface attachment, membrane penetration, and absence of lipid interactions. Application of complementary bioanalytical techniques corroborated the interpretation of the colorimetric data. Different pharmaceutical co...Continue Reading

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Citations

Apr 2, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Aharon AzaguryJoseph Kost
Jan 6, 2007·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Gøril Eide FlatenMartin Brandl
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Feb 6, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Aneta PokornaJosef Jampilek
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Jul 16, 2009·Molecular BioSystems·Raz Jelinek, Liron Silbert
Jul 8, 2020·International Journal of Molecular Sciences·Jinsha Liu, Sepideh Afshar
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Oct 13, 2006·Journal of the American Chemical Society·Sofiya KolushevaRaz Jelinek
Oct 29, 2021·The Journal of Physical Chemistry. B·Jiangtao Zhao, Kaori Sugihara

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