Leveraging bile solubilization of poorly water-soluble drugs by rational polymer selection.
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Authors
Schlauersbach, JonasHanio, Simon
Lenz, Bettina
Vemulapalli, Sahithya P B
Griesinger, Christian
Pöppler, Ann-Christin
Harlacher, Cornelius
Galli, Bruno
Meinel, Lorenz
Issue Date
2020-12-15
Metadata
Show full item recordAbstract
Poorly water-soluble drugs frequently solubilize into bile colloids and this natural mechanism is key for efficient bioavailability. We tested the impact of pharmaceutical polymers on this solubilization interplay using proton nuclear magnetic resonance spectroscopy, dynamic light scattering, and by assessing the flux across model membranes. Eudragit E, Soluplus, and a therapeutically used model polymer, Colesevelam, impacted the bile-colloidal geometry and molecular interaction. These polymer-induced changes reduced the flux of poorly water-soluble and bile interacting drugs (Perphenazine, Imatinib) but did not impact the flux of bile non-interacting Metoprolol. Non-bile interacting polymers (Kollidon VA 64, HPMC-AS) neither impacted the flux of colloid-interacting nor colloid-non-interacting drugs. These insights into the drug substance/polymer/bile colloid interplay potentially point towards a practical optimization parameter steering formulations to efficient bile-solubilization by rational polymer selection.Citation
J Control Release. 2020 Dec 15;330:36-48. doi: 10.1016/j.jconrel.2020.12.016. Epub ahead of print.Affiliation
HIRI, Helmholtz-Institut für RNA-basierte Infektionsforschung, Josef-Shneider Strasse 2, 97080 Würzburg, Germany.Publisher
ElsevierPubMed ID
33333120Type
ArticleLanguage
enEISSN
1873-4995ae974a485f413a2113503eed53cd6c53
10.1016/j.jconrel.2020.12.016
Scopus Count
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- Creative Commons
Except where otherwise noted, this item's license is described as Attribution-NonCommercial-NoDerivatives 4.0 International
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