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dc.contributor.authorEndres, Sebastian
dc.contributor.authorKaraev, Emil
dc.contributor.authorHanio, Simon
dc.contributor.authorSchlauersbach, Jonas
dc.contributor.authorKraft, Christian
dc.contributor.authorRasmussen, Tim
dc.contributor.authorLuxenhofer, Robert
dc.contributor.authorBöttcher, Bettina
dc.contributor.authorMeinel, Lorenz
dc.contributor.authorPöppler, Ann-Christin
dc.date.accessioned2021-11-19T15:03:10Z
dc.date.available2021-11-19T15:03:10Z
dc.date.issued2021-08-10
dc.identifier.citationJ Colloid Interface Sci. 2022 Jan 15;606(Pt 2):1179-1192. doi: 10.1016/j.jcis.2021.08.040. Epub 2021 Aug 10.en_US
dc.identifier.pmid34487937
dc.identifier.doi10.1016/j.jcis.2021.08.040
dc.identifier.urihttp://hdl.handle.net/10033/623100
dc.description.abstractMany drugs and drug candidates are poorly water-soluble. Intestinal fluids play an important role in their solubilization. However, the interactions of intestinal fluids with polymer excipients, drugs and their formulations are not fully understood. Here, diffusion ordered spectroscopy (DOSY) and nuclear Overhauser effect spectroscopy (NOESY), complemented by cryo-TEM were employed to address this. Efavirenz (EFV) as model drug, the triblock copolymers Pluronic® F-127 (PF127) and poly(2-oxazoline) based pMeOx-b-pPrOzi-b-pMeOx (pOx/pOzi) and their respective formulations were studied in simulated fed-state intestinal fluid (FeSSIF). For the individual polymers, the bile interfering nature of PF127 was confirmed and pure pOx/pOzi was newly classified as non-interfering. A different and more complex behaviour was however observed if EFV was involved. PF127/EFV formulations in FeSSIF showed concentration dependent aggregation with separate colloids at low formulation concentrations, a merging of individual particles at the solubility limit of EFV in FeSSIF and joint aggregates above this concentration. In the case of pOx/pOzi/EFV formulations, coincident diffusion coefficients for pOx/pOzi, lipids and EFV indicate joint aggregates across the studied concentration range. This demonstrates that separate evaluation of polymers and drugs in biorelevant media is not sufficient and their mixtures need to be studied to learn about concentration and composition dependent behaviour.en_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 International*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/*
dc.subjectBile colloidsen_US
dc.subjectConcentation dependent interactionen_US
dc.subjectDOSYen_US
dc.subjectDrug-Polymer Formulationsen_US
dc.titleConcentration and composition dependent aggregation of Pluronic- and Poly-(2-oxazolin)-Efavirenz formulations in biorelevant media.en_US
dc.typeArticleen_US
dc.identifier.eissn1095-7103
dc.contributor.departmentHIRI, Helmholtz-Institut für RNA-basierte Infektionsforschung, Josef-Shneider Strasse 2, 97080 Würzburg, Germany.en_US
dc.identifier.journalJournal of colloid and interface scienceen_US
dc.source.volume606
dc.source.issuePt 2
dc.source.beginpage1179
dc.source.endpage1192
refterms.dateFOA2021-11-19T15:03:10Z
dc.source.journaltitleJournal of colloid and interface science
dc.source.countryUnited States


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