Biorelevant media for transport experiments in the Caco-2 model to evaluate drug absorption in the fasted and the fed state and their usefulness

Biomimetic PVPA in vitro model for estimation of the intestinal drug permeability using fasted and fed state simulated intestinal fluids

“…Since griseofulvin is a nonionizable drug, the decreased permeability is most probably due to the drug associated within the micelles thereby decreasing the free fraction of the drug. The following rank order of permeability: PB > FaSSIF > FeSSIF has also been reported for other BCS II drugs (Markopoulos et al, 2014). Similar results for griseofulvin obtained using the PVPAo model has also been reported (Fischer et al, 2012).…”

“…This is as expected since drug compounds belonging to the BCS III, like acyclovir, are less likely to undergo an interaction with colloidal systems (Markopoulos et al, 2014).…”

“…On the other hand, regarding the PAMPA model the knowledge of the effect of biorelevant media is very limited (Markopoulos et al, 2014). This further highlights the PVPA models' advantages in drug permeability screening.…”

“…The use of FaSSIF and FeSSIF in other permeability models such as the Caco-2 cell model has also been reported and it was shown that the presence of these media (in original or modified form) neither affected the cell viability or the barrier integrity (Fossati et al, 2008;Ingels et al, 2004;Ingels et al, 2002;Kataoka et al, 2006;Markopoulos et al, 2014;Patel et al, 2006). On the other hand, regarding the PAMPA model the knowledge of the effect of biorelevant media is very limited (Markopoulos et al, 2014).…”

“…PAMPA generally consists of a filter support covered with phospholipids in organic solvents, which allows for medium-to high-throughput screening of drug permeability. However, lack of resemblance with the biological membrane structure, few reports on use in permeability screening from different formulations and limited knowledge on use of more biorelevant media is placing a limitation on this model (Flaten et al, 2006b;Markopoulos et al, 2014).…”