Four cation-selective transporters contribute to apical uptake and accumulation of metformin in Caco-2 cell monolayers.

ABSTRACT: Metformin is the frontline therapy for type II diabetes mellitus. The oral bioavailability of metformin is unexpectedly high, between 40 and 60%, given its hydrophilicity and positive charge at all physiologic pH values. Previous studies in Caco-2 cell monolayers, a cellular model of the human intestinal epithelium, showed that during absorptive transport metformin is taken up into the cells via transporters in the apical (AP) membrane; however, predominant transport to the basolateral (BL) side occurs via the paracellular route because intracellular metformin cannot egress across the BL membrane. Furthermore, these studies have suggested that the AP transporters can contribute to intestinal accumulation and absorption of metformin. Transporter-specific inhibitors as well as a novel approa

SUBMITTER: Han TK 

PROVIDER: S-EPMC4352590 | biostudies-literature | 2015 Mar

REPOSITORIES: biostudies-literature