Leveraging bile solubilization of poorly water-soluble drugs by rational polymer selection.
Cast your vote
You can rate an item by clicking the amount of stars they wish to award to this item.
When enough users have cast their vote on this item, the average rating will also be shown.
Your vote was cast
Thank you for your feedback
Thank you for your feedback
Vemulapalli, Sahithya P B
MetadataShow full item record
AbstractPoorly 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.
CitationJ Control Release. 2020 Dec 15;330:36-48. doi: 10.1016/j.jconrel.2020.12.016. Epub ahead of print.
AffiliationHIRI, Helmholtz-Institut für RNA-basierte Infektionsforschung, Josef-Shneider Strasse 2, 97080 Würzburg, Germany.
The following license files are associated with this item:
- Creative Commons
Except where otherwise noted, this item's license is described as Attribution-NonCommercial-NoDerivatives 4.0 International
- Drug-Induced Dynamics of Bile Colloids.
- Authors: Hanio S, Schlauersbach J, Lenz B, Spiegel F, Böckmann RA, Schweins R, Nischang I, Schubert US, Endres S, Pöppler AC, Brandl FP, Smit TM, Kolter K, Meinel L
- Issue date: 2021 Mar 2
- Geometrical and Structural Dynamics of Imatinib within Biorelevant Colloids.
- Authors: Wiest J, Saedtler M, Böttcher B, Grüne M, Reggane M, Galli B, Holzgrabe U, Meinel L
- Issue date: 2018 Oct 1
- Impact of Gut Microbiota-Mediated Bile Acid Metabolism on the Solubilization Capacity of Bile Salt Micelles and Drug Solubility.
- Authors: Enright EF, Joyce SA, Gahan CG, Griffin BT
- Issue date: 2017 Apr 3
- Probing the molecular interactions between pharmaceutical polymeric carriers and bile salts in simulated gastrointestinal fluids using NMR spectroscopy.
- Authors: Pigliacelli C, Belton P, Wilde P, Qi S
- Issue date: 2019 Sep 1
- Polymer Type Impacts Amorphous Solubility and Drug-Rich Phase Colloidal Stability: A Mechanistic Study Using Nuclear Magnetic Resonance Spectroscopy.
- Authors: Ueda K, Taylor LS
- Issue date: 2020 Apr 6