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

نویسندگان

چکیده

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 solubilization interplay using proton nuclear magnetic resonance spectroscopy, dynamic light scattering, by assessing flux across model membranes. Eudragit E, Soluplus, a therapeutically used polymer, Colesevelam, impacted bile-colloidal geometry molecular interaction. These polymer-induced changes reduced poorly interacting (Perphenazine, Imatinib) but did not non-interacting Metoprolol. Non-bile (Kollidon VA 64, HPMC-AS) neither colloid-interacting nor colloid-non-interacting drugs. insights drug substance/polymer/bile colloid potentially point towards practical optimization parameter steering formulations to bile-solubilization rational polymer selection.

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ژورنال

عنوان ژورنال: Journal of Controlled Release

سال: 2021

ISSN: ['1873-4995', '0168-3659']

DOI: https://doi.org/10.1016/j.jconrel.2020.12.016