Using Human Plasma as an Assay Medium in Caco-2 Studies Improves Mass Balance for Lipophilic Compounds.

ABSTRACT:

Purpose

To examine the utility of human plasma as an assay medium in Caco-2 permeability studies to overcome poor mass balance and inadequate sink conditions frequently encountered with lipophilic compounds.

Methods

Caco-2 permeability was assessed for reference compounds with known transport mechanisms using either pH 7.4 buffer or human plasma as the assay medium in both the apical and basolateral chambers. When using plasma, P_app values were corrected for the unbound fraction in the donor chamber. The utility of the approach was assessed by measuring the permeability of selected antimalarial compounds using the two assay media.

Results

Caco-2 cell monolayer integrity and P-gp transporter function were unaffected by the presence of human plasma in the don

SUBMITTER: Katneni K 

PROVIDER: S-EPMC6156755 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature