Use of simulated intestinal fluid for Caco-2 permeability assay of lipophilic drugs

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

“…Indomethacin and griseofulvin showed increased recovery rates in the presence of FaSSIF and FeSSIF indicating the media's contribution in preventing the drug adsorption to the experimental materials and/or entrapment of the compounds into the membrane. Similar observations regarding the impact of the simulated intestinal fluids on the recovery have been reported earlier (Fischer et al, 2012;Fossati et al, 2008;Ingels et al, 2004). According to those reports, the lipophilic drugs with moderate to high log p values (above 2.5) showed increased recovery in the presence of simulated intestinal fluids as compared to the buffers, in agreement with our findings.…”

“…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).…”

Towards Prediction of In Vivo Intestinal Absorption Using a 96-Well Caco-2 Assay

“…In reality contradictory results were observed (e.g., lower recovery rate or permeability for bare insert plates than in the presence of membrane or monolayer). Indeed, a recent publication 33 confirmed that only a small fraction of test compounds (7 of 18, or 39%) exhibited higher average recovery rate in the cell-free plates than Caco-2 plates. The above observation should not be surprising as compound may not properly diffuse through the filter pores of the bare plate, possibly due to surface tension and poor wettability.…”

“…As expected, standard compounds typically have better mass balance or recovery closer to 100% in cellular assays compared to discovery compounds due to their favorable physicochemical properties. 14,33 Most standards in Table 1 exhibited ideal recovery 80-120% (data not reported). In contrast, when we examined 8000 NCE mass balance results over 2 years from the described Caco-2 assay, approximately 13% were found to have %recovery <30 (Tab.…”

Síntese e caracterização de derivados 3,6-<i>O</i>,<i>O</i>\'-dimiristoil quitosana para encapsulação e liberação de fármacos antitumorais

“…Nesse tipo de ensaio, quando as células Caco-2 são mantidas em condições adequadas de cultivo, elas são capazes de crescer e formar uma monocamada de células cilíndricas polarizadas, apresentando microvilosidades na borda apical do transwell, junções oclusivas entre as células adjacentes, enzimas hidrolisantes e sistemas de transporte mediados por portadores de açúcares, aminoácidos e diversos fármacos (INGELS et al, 2002;FOSSATI et al, 2008).…”