Biological, Pharmaceutical, and Analytical Considerations with Respect to the Transport Media Used in the Absorption Screening System, Caco-2

Water-soluble organic solubilizers for in vitro drug delivery studies with respiratory epithelial cells: Selection based on various toxicity indicators

“…The use of reasonably high concentrations of solubilizers for in vitro permeation studies with Caco-2 and other epithelial cells have been reported (Ingels & Augustijns, 2003;Hamid et al, 2009). The results of our study were in agreement with some of the published data for DMSO, Cremophor EL, and PEG 400, but different for DMA and MPH.…”

“…Calu-3 cell line was selected as a model for the respiratory system because of its wide range of applications as an in vitro drug delivery model (Forbes & Ehrhardt, 2005). The chosen solubilizers have been used for solubilizing many pharmaceutical compounds (Ingels & Augustijns, 2003).…”

“…For instance, Hamid et al (2009) reported that up to 10% PEG 400, DMSO, and Cremophor ® EL were suitable for drug delivery studies with Caco-2 cells and isolated rat intestine. Ingels and Augustijns (2003) recommended the use of 3% DMA and 2.5% MPH for in vitro studies with Caco2 cells. The disparity between the studies from which the recommendation was made and our data may be explained by differences in toxicity indices.…”

Applications of cell culture studies in pharmaceutical technology

“…These differences may affect the permeability of compounds which are specific to transporters showing different expression profiles 57 . TEER values and permeability values of Caco-2 from different laboratories can be different due to varying culture conditions 60,61,62 . Although the transepithelial electrical resistance (TEER) of small intestine is estimated to be in the range of 25-40 Ω cm .…”

Instrumented In Vitro Approaches to Assess Epithelial Permeability of Drugs from Pharmaceutical Formulations

“…Permeability assessment through Caco-2 monolayers is routinely carried out using Krebs Ringer buffer (KRB), Krebs bicarbonate Ringer buffer (KBR), or Hank's balanced salt solution (HBSS), though those might pose too restrictive conditions for low-soluble compounds, due to the lack of lipids and surface active ingredients and their excessive amount of counter-ions. A shortcoming for low-solubility compounds can generally be seen in the addition of either Dimethylsulfoxide or other cosolvents (a comprehend review of applied substance together with concentrations is comprised in [36]). For more comparable in vivo permeation conditions in Caco-2 assays, Ingels et al [37] recommend to use FaSSIF on the apical side, while basolaterally an analytical-friendly buffer, such as HBSS, may be the best choice.…”