Mucin-Protected Caco-2 Assay to Study Drug Permeation in the Presence of Complex Biorelevant Media.

ABSTRACT: The poor solubility and permeability of compounds beyond Lipinski's Rule of Five (bRo5) are major challenges for cell-based permeability assays. Due to their incompatibility with gastrointestinal components in biorelevant media, the exploration of important questions addressing food effects is limited. Thus, we established a robust mucin-protected Caco-2 assay to allow the assessment of drug permeation in complex biorelevant media. To do that, the assay conditions were first optimized with dependence of the concentration of porcine mucin added to the cells. Mucin-specific effects on drug permeability were evaluated by analyzing cell permeability values for 15 reference drugs (BCS class I-IV). Secondly, a sigmoidal relationship between mucin-dependent permeability and fraction absorbed in h

SUBMITTER: Ye D 

PROVIDER: S-EPMC9032137 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature