TY  - JOUR
A1  - Schlauersbach, Jonas
A1  - Hanio, Simon
A1  - Lenz, Bettina
A1  - Vemulapalli, Sahithya P. B.
A1  - Griesinger, Christian
A1  - Pöppler, Ann-Christin
A1  - Harlacher, Cornelius
A1  - Galli, Bruno
A1  - Meinel, Lorenz
T1  - Leveraging bile solubilization of poorly water-soluble drugs by rational polymer selection
T2  - Journal of Controlled Release
N2  - 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.
KW  - polymer drug interaction
KW  - flux
KW  - bile salt
KW  - simulated intestinal fluid
KW  - colloid
Y1  - 2021
UR  - https://opus.bibliothek.uni-wuerzburg.de/frontdoor/index/index/docId/29695
UR  - https://nbn-resolving.org/urn:nbn:de:bvb:20-opus-296957
VL  - 330
ER  -