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  Leveraging bile solubilization of poorly water-soluble drugs by rational polymer selection

Schlauersbach, J., Hanio, S., Lenz, B., Vemulapalli, S. P., Griesinger, C., Pöppler, A.-C., et al. (2021). Leveraging bile solubilization of poorly water-soluble drugs by rational polymer selection. Journal of Controlled Release, 330, 36-48. doi:10.1016/j.jconrel.2020.12.016.

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 Creators:
Schlauersbach, J., Author
Hanio, S., Author
Lenz, B., Author
Vemulapalli, S. P.1, Author           
Griesinger, C.2, Author                 
Pöppler, A.-C., Author
Harlacher, C., Author
Galli, B., Author
Meinel, L., Author
Affiliations:
1Department of NMR Based Structural Biology, MPI for Biophysical Chemistry, Max Planck Society, ou_578567              
2Department of NMR Based Structural Biology, MPI for biophysical chemistry, Max Planck Society, ou_578567              

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Free keywords: Polymer drug interaction; Flux; Bile salt; Simulated intestinal fluid; Colloid
 Abstract: 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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Language(s): eng - English
 Dates: 2020-12-152021-02-10
 Publication Status: Published in print
 Pages: -
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1016/j.jconrel.2020.12.016
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Title: Journal of Controlled Release
Source Genre: Journal
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Publ. Info: -
Pages: - Volume / Issue: 330 Sequence Number: - Start / End Page: 36 - 48 Identifier: -