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dc.contributor.authorHanio, Simon
dc.contributor.authorSchlauersbach, Jonas
dc.contributor.authorLenz, Bettina
dc.contributor.authorSpiegel, Franziska
dc.contributor.authorBöckmann, Rainer A
dc.contributor.authorSchweins, Ralf
dc.contributor.authorNischang, Ivo
dc.contributor.authorSchubert, Ulrich S
dc.contributor.authorEndres, Sebastian
dc.contributor.authorPöppler, Ann-Christin
dc.contributor.authorBrandl, Ferdinand P
dc.contributor.authorSmit, Theo M
dc.contributor.authorKolter, Karl
dc.contributor.authorMeinel, Lorenz
dc.date.accessioned2021-03-09T12:36:07Z
dc.date.available2021-03-09T12:36:07Z
dc.date.issued2021-02-15
dc.identifier.citationLangmuir. 2021 Mar 2;37(8):2543-2551. doi: 10.1021/acs.langmuir.0c02282. Epub 2021 Feb 15.en_US
dc.identifier.pmid33587852
dc.identifier.doi10.1021/acs.langmuir.0c02282
dc.identifier.urihttp://hdl.handle.net/10033/622775
dc.description.abstractBile colloids containing taurocholate and lecithin are essential for the solubilization of hydrophobic molecules including poorly water-soluble drugs such as Perphenazine. We detail the impact of Perphenazine concentrations on taurocholate/lecithin colloids using analytical ultracentrifugation, dynamic light scattering, small-angle neutron scattering, nuclear magnetic resonance spectroscopy, coarse-grained molecular dynamics simulations, and isothermal titration calorimetry. Perphenazine impacted colloidal molecular arrangement, structure, and binding thermodynamics in a concentration-dependent manner. At low concentration, Perphenazine was integrated into stable and large taurocholate/lecithin colloids and close to lecithin. Integration of Perphenazine into these colloids was exothermic. At higher Perphenazine concentration, the taurocholate/lecithin colloids had an approximately 5-fold reduction in apparent hydrodynamic size, heat release was less exothermic upon drug integration into the colloids, and Perphenazine interacted with both lecithin and taurocholate. In addition, Perphenazine induced a morphological transition from vesicles to wormlike micelles as indicated by neutron scattering. Despite these surprising colloidal dynamics, these natural colloids successfully ensured stable relative amounts of free Perphenazine throughout the entire drug concentration range tested here. Future studies are required to further detail these findings both on a molecular structural basis and in terms of in vivo relevance.en_US
dc.language.isoenen_US
dc.publisherAmerican Society for Chemistry (ACS)en_US
dc.rightsAttribution-NonCommercial-ShareAlike 4.0 International*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-sa/4.0/*
dc.titleDrug-Induced Dynamics of Bile Colloids.en_US
dc.typeArticleen_US
dc.identifier.eissn1520-5827
dc.contributor.departmentHIRI, Helmholtz-Institut für RNA-basierte Infektionsforschung, Josef-Shneider Strasse 2, 97080 Würzburg, Germany.en_US
dc.identifier.journalLangmuir : the ACS journal of surfaces and colloidsen_US
dc.source.volume37
dc.source.issue8
dc.source.beginpage2543
dc.source.endpage2551
dc.source.journaltitleLangmuir : the ACS journal of surfaces and colloids
dc.source.countryUnited States


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