References
Audus KA, Borchardt RT. Characterization of an in vitro blood–brain barrier model system for studying drug transport and metabolism. Pharm Res. 1986;3:81–7.
Osiecka I, Borchardt RT, Fix JA, Gardner CA, Porter PA. In vitro drug absorption models. I. Brush border membrane vesicles, isolated mucosal cells and everted intestinal rings: characterization and salicylate accumulation. Pharm Res. 1985;2:284–93.
Porter PA, Osiecka I, Borchardt RT, Fix JA, Frost L, Gardner CA. In vitro drug absorption models. II. Salicylate, cefoxitin, α-methyldopa and theophylline uptake in cells and rings: correlation with in vivo bioavailability. Pharm Res. 1985;2:293–8.
Osiecka I, Cortese M, Porter PA, Borchardt RT, Fix JA, Gardner CR. Intestinal absorption of α-methyldopa: in vitro mechanistic studies in rat small intestinal segments. J Pharmacol Exp Ther. 1987;242:443–9.
Leibovitz A, Stinson JC, McCombs WB, McCoy CE, Mazur KC, Mabry ND. Classification of human colorectal adenocarcinoma cell line. Cancer Res. 1976;36:4562–9.
Pinto M, Appay M-D, Simon-Assmann P, Chevalier G, Dracopoli N, Fogh J, et al. Enterocytic differentiation of cultured human colon cancer cells by replacement of glucose by galactose in the medium. Biol Cell. 1982;44:193–6.
Pinto M, Robine-Leon S, Appay M-D, Kedinger M, Triadou N, Dussaulx E, et al. Enterocyte-like differentiation and polarization of the human colon carcinoma cell line Caco-2 in culture. Biol Cell. 1983;47:323–30.
Hidalgo IJ, Raub TJ, Kuentzel SL, Borchardt RT. Characterization of the Caco-2 cell line as an intestinal epithelial model system. FASEB J. 1988;2:A734. Abst. #2539.
Hidalgo IJ, Kato A, Borchardt RT. Epidermal growth factor (EGF) binding in a human colon carcinoma cell-line (Caco-2). FASEB J. 1989;3:A899. Abst. #3906.
Hidalgo IJ, Borchardt RT, Raub TJ. Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology. 1989;96:736–49.
Hidalgo IJ, Borchardt RT. Transport of taurocholic acid in an intestinal epithelial model system (Caco-2 cell). Pharm Res. 1988;5:S-110. Abst. #949.
Hidalgo IJ, Borchardt RT. Amino acid transport in a novel model system of the intestinal epithelium (Caco-2 cell). Pharm Res. 1988;5:S-110. Abst. #PD950.
Hidalgo IJ, Hillgren KM, Grass GM, Borchardt RT. Characterization of the aqueous boundary layer in Caco-2 cells using a novel diffusion cell. Pharm Res. 1989;6:S-114. Abst. #PD950.
Hidalgo IJ, Borchardt RT. Polarity of bile acid uptake and efflux in an intestinal epithelial cell line. Pharm Res. 1989;6:S-115. Abst. #PD953.
Hidalgo IJ, Kato A, Borchardt RT. Epidermal growth factor (EGF) binding in a human colon carcinoma cell line (Caco-2). Biochem Biophys Res Commun. 1989;158:317–24.
Hidalgo IJ, Borchardt RT. Transport of a large neutral amino acid (phenylalanine) in a human intestinal epithelial cell line: Caco-2. Biochim Biophys Acta. 1028;25–30:1990.
Hidalgo IJ, Borchardt RT. Transport of bile acids in a human intestinal epithelial cell line: Caco-2. Biochim Biophys Acta. 1035;97–103:1990.
Audus K, Bartel R, Hidalgo I, Borchardt RT. The use of cultured epithelial and endothelial cells for drug transport and metabolism studies. Pharm Res. 1990;7:435–51.
Hidalgo IJ, Borchardt RT. Carrier-mediated transport of bile acids and amino acids in Caco-2 cells. In: Wilson G, Davis SS, Illum L, editors. Pharmaceutical applications of cell and tissue culture to drug transport. New York: Plenum; 1991. p. 77–92.
Borchardt RT, Hidalgo IJ, Hillgren KM, Hu M. Pharmaceutical applications of cell culture—an overview. In: Wilson G, Davis SS, Illum L, editors. Pharmaceutical applications of cell and tissue culture to drug transport. New York: Plenum; 1991. p. 1–14.
Hidalgo IJ, Hillgren KM, Grass GM, Borchardt RT. Characterization of the unstirred water layer in Caco-2 cells using a novel diffusion cell. Pharm Res. 1991;8:223–7.
Artursson P. Epithelial transport of drugs. I. A model for studying the transport of drugs (β-blocking agents) over an intestinal epithelial cell line (Caco-2). J Pharm Sci. 1990;79:476–82.
Artursson P, Magnusson C. Epithelial transport of drugs 2. Effect of extracellular calcium on the transport of hydrophilic and lipophilic drugs (ß-blocking agents) over an intestinal epithelial (Caco-2) cell line. J Pharm Sci. 1990;79:595–600.
Karlsson J, Artursson P. A method for the determination of cellular permeability coefficients and aqueous boundary layer thickness in monolayers of intestinal epithelial (Caco-2) cells grown in permeable filter chambers. Int J Pharm. 1991;71:55–64.
Artursson P, Karlsson J. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem Biophys Res Commun. 1991;175:880–5.
Hillgers AR, Conradi RA, Burton PS. Caco-2 cell monolayers as a model for drug transport across the intestinal mucosa. Pharm Res. 1990;7:902–10.
Hillgers AR, Conradi RA, Ho NF, Burton PS. The influence of peptide structure on transport across Caco-2 cells. Pharm Res. 1991;8:1453–60.
Author information
Authors and Affiliations
Corresponding author
Additional information
Editor: Ho-Leung Fung
This manuscript was written with the knowledge and input of Ismael J. Hidalgo and Thomas J. Raub, who were coauthors of the 1989 Gastroenterology paper describing for the first time Caco-2 cell monolayers as a cell culture model of the intestinal mucosa.
Rights and permissions
About this article
Cite this article
Borchardt, R.T. Hidalgo, I. J., Raub, T. J., and Borchardt, R. T.: Characterization of the Human Colon Carcinoma Cell Line (Caco-2) as a Model System for Intestinal Epithelial Permeability, Gastroenterology, 96, 736–749, 1989—The Backstory. AAPS J 13, 323–327 (2011). https://doi.org/10.1208/s12248-011-9283-8
Received:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1208/s12248-011-9283-8