Journal
JOURNAL OF CONTROLLED RELEASE
Volume 330, Issue -, Pages 36-48Publisher
ELSEVIER
DOI: 10.1016/j.jconrel.2020.12.016
Keywords
Polymer drug interaction; Flux; Bile salt; Simulated intestinal fluid; Colloid
Funding
- Novartis Pharma AG
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Pharmaceutical polymers can impact the solubilization of poorly water-soluble drugs into bile colloids, affecting the flux of certain drugs while not impacting others. Understanding this interplay between drug substance, polymer, and bile colloid may lead to more efficient bile-solubilization formulations through rational polymer selection.
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.
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