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Abstract

Human colon adenocarcinoma (Caco-2) cells, when grown on semipermeable filters, spontaneously differentiate in culture to form confluent monolayers which both structurally and functionally resemble the small intestinal epithelium. Because of this property they show promise as a simple, in vitro model for the study of drug absorption and metabolism during absorption in the intestinal mucosa. In the present study, the transport of several model solutes across Caco-2 cell monolayers grown in the Transwell diffusion cell system was examined. Maximum transport rates were found for the actively transported substance glucose and the lipophilic solutes testosterone and salicyclic acid. Slower rates were observed for urea, hippurate, and saliylate anions and were correlated with the apparent partition coefficient of the solute. These results are similar to what is found with the same compounds in other, in vivo absorption model systems. It is concluded that the Caco-2 cell system may give useful predictions concerning the oral absorption potential of new drug substances.

A Microfluidic System to Evaluate Intestinal Absorption

“…[1][2][3] The Caco-2 cells form a single cell layer connected via tight junctions, thus affording the layer an ability to selectively permeate certain molecules. 4 Although existing systems are easy to deal with for scientists, they require large amounts of cells, reagents, samples, and culture media for an assay, which take a long time to test. Moreover, a more rapid evaluation method with lower costs and a simpler procedure is required for efficient drug screening research.…”

Determination ofin vitro permeability of drug candidates through a Caco-2 cell monolayer by liquid chromatography/tandem mass spectrometry

“…4,5 Thus, Caco-2 cell lines have been widely used as an in vitro model for oral drug absorption, drug interaction and metabolism studies. 6 -13 In our laboratory Caco-2 cells are used as an in vitro drug absorption model for identifying compounds with high permeability and absorption potential. This model also has been used by other laboratories for 'high'-throughput screening in drug discovery.…”

Polymeric microcontainers improve oral bioavailability of furosemide

“…Cell culture models are one of many methods used to study intestinal absorption (Patel et al, 2006;Pretorius and Bouic, 2009). The Caco-2 cell line is an epithelial cell line originating from a human colonic adenocarcinoma, which represents many of the characteristics and functions found in the epithelium of the small intestine (tight junctions, microvilli, growth factor receptors, and major drug metabolizing enzymes) (Berginc et al, 2012;Hidalgo et al, 1989;Hilgers et al, 1990). The Caco-2 cell model has become a useful in vitro tool to predict permeability and absorption of drugs across the small intestinal membrane, and is a valuable set-up to be employed during the development of oral drug delivery systems (Hidalgo et al, 1989).…”