Caco-2/TC7 cell line characterization for intestinal absorption: How reliable is this in vitro model for the prediction of the oral dose fraction absorbed in human?

Toxicology in Vitro

Volumn 25, Issue 1, 2011, Pages 13-20

  Turco, Laura ^a   Catone, Tiziana ^a   Caloni, Francesca ^b   Consiglio, Emma Di ^a   Testai, Emanuela ^a   Stammati, Annalaura ^a  

^a ISTITUTO SUPERIORE DI SANITÀ   (Italy)

^b UNIVERSITY OF MILAN   (Italy)

Author keywords

Caco 2 cells; Intestinal absorption; Predictive method

Indexed keywords

ACETYLSALICYLIC ACID; ATENOLOL; ATROPINE; CADMIUM CHLORIDE; CAFFEINE; CARBAMAZEPINE; CIMETIDINE; COLCHICINE; CYCLOHEXIMIDE; DIAZEPAM; DIGOXIN; FURAZOLIDONE; IMIPRAMINE; LITHIUM SULFATE; MALATHION; MANNITOL; NICOTINE; ORPHENADRINE; PARACETAMOL; PARAOXON; PARATHION; PENTACHLOROPHENOL; PHENOBARBITAL; PROPRANOLOL; VALPROIC ACID; VERAPAMIL; WARFARIN;

ACTIVE TRANSPORT; ADSORPTION KINETICS; ARTICLE; CELL COMPARTMENTALIZATION; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; CONCENTRATION RESPONSE; CONTROLLED STUDY; CYTOTOXICITY TEST; HUMAN; HUMAN CELL; IN VITRO STUDY; INTESTINE ABSORPTION; MATHEMATICAL COMPUTING; MATHEMATICAL MODEL; MEMBRANE FILTER; MOLECULAR CLONING; MOLECULAR MODEL; PASSIVE TRANSPORT; PROTEIN METABOLISM; PROTEIN TRANSPORT; REACTION TIME; RELIABILITY;

ADMINISTRATION, ORAL; ALGORITHMS; CACO-2 CELLS; CLONE CELLS; ENTEROCYTES; HUMANS; INTESTINAL ABSORPTION; PERMEABILITY; REPRODUCIBILITY OF RESULTS;

EID: 78650517988     PISSN: 08872333     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.tiv.2010.08.009     Document Type: Article

References (65)

1. Artursson P. Cell cultures as models for drug absorption across the intestinal mucosa. Crit. Rev. Ther. Drug Carrier Syst. 1991, 8:305-330.
2. Artursson P., Lindmark T., Davis S., Illum L. Effect of chitosan on the permeability of monolayers of intestinal epithelial cells (Caco-2). Pharm. Res. 1994, 11:1358-1361.
3. Artursson P., Palm K., Luthman K. Caco-2 monolayers in experimental and theoretical predictions of drug transport. Adv. Drug Del. Rev. 2001, 46:27-43.
4. Balimane P.V., Chong S., Morrison R.A. Current methodologies used for evaluation of intestinal permeability and absorption. J. Pharmacol. Toxicol. Methods 2000, 44:301-312.
5. Balon K., Riebesehl B.U., Muller B.W. Drug liposome partitioning as a tool for the prediction of human passive intestinal absorption. Pharm. Res. 1999, 16:882-888.
6. Bispo M.S., Veloso M.C.C., Pinheiro H.L.C., De Oliveira R.F.S., Reis J.O.N., De Andrade J.B. Simultaneous determination of caffeine, theobromine, and theophylline by high-performance liquid chromatography. J. Chromatogr. Sci. 2002, 40:45-48.
7. Briske-Anderson M.J., Finley J.W., Newman S.M. The influence of culture time and passage member on the morphological and physiological development of Caco-2 cells. Proc. Soc. Exp. Biol. Med. 1997, 214:248-257.
8. Brown L.W. High-pressure liquid chromatographic determination of cycloheximide in ointment and suspension formulations. J. Pharm. Sci. 2006, 67:669-672.
9. Buratti F.M., D'Aniello A., Volpe M.T., Meneguz A., Testai E. Malathion bioactivation in the human liver: the contribution of different cytochrome P450 isoforms. Drug Metab. Dispos. 2005, 33(3):295-302.
10. Caro I., Boulenc X., Rousset M., Meunier V., Bourrié M., Julian B., Joyeux H., Roques C., Berger Y., Zweibaum A., Fabre G. Characterization of a newly isolated Caco-2 clone (TC-7), as a model of transport processes and biotransformation of drugs. Int. J. Pharmacol. 1995, 116:147-158.
11. Chantret I., Rodolosse A., Barbat A., Dussaulx E., Brot-Laroche E., Zweibaum A., Rousset M. Differential expression of sucrase-isomaltase in clones isolated from early and late passages of the cell line Caco-2: evidence for glucose-dependent negative regulation. J. Cell Sci. 1994, 107(Pt 1):213-225.
12. Delie F., Rubas W. A human colonic cell line sharing similarities with enterocytes as a model to examine oral absorption: advantages and limitations of the Caco-2 model. Crit. Rev. Ther. Drug Carrier Syst. 1997, 14:221-286.
13. Djuv, A., Nilsen, G., 2008. Caco-2 cell methodology and inhibition of the P-glycoprotein transport of digoxin by Aloe vera juice. Phytotherapy Research, Published Online in Wiley InterScience. doi:10.1002/ptr.2536. http://www.interscience.wiley.com.
14. Therapeutical Drugs 1999, Churchill Livingstone. second ed. C. Dolly (Ed.).
15. Eyer F., Jung N., Neuberger H., Witte A., Poethko T., Henke J., Zilker T. Seromucosal transport of intravenously administered carbamazepine is not enhanced by oral doses of activated charcoal in rats. Basic Clin. Pharmacol. Toxicol. 2007, 102:337-346.
16. Fagerholm U. Prediction of human pharmacokinetics-gastrointestinal absorption. J. Pharm. Pharmacol. 2007, 59:905-916.
17. FDA, 2000. Guidance for Industry: Waiver of in vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System. US Food and Drug Administration, Center for Drug Evaluation and Research, USA. http://www.fda.gov/cder/guidance/3618fnl.pdf.
18. Foxenberg R.J., McGarrigl B.P., Knaak J.B., Kostyniak P.J., Olson J.R. Human hepatic cytochrome P450-specific metabolism of parathion and chlorpyrifos. Drug Metab. Dispos. 2007, 35(235):189-193.
19. Grès M.C., Julian B., Bourrié M., Meunier V., Roques C., Berger M., Boulenc X., Berger Y., Fabre G. Correlation between oral drug absorption in humans and apparent drug permeability in TC-7 cells, a human epithelial intestinal cell line: comparison with the parental Caco-2 cell line. Pharm. Res. 1998, 15:726-733.
20. Guillaume Y., Guinchard C. Marked differences between acetonitrile/water and methanol/watermobile phase system on the thermodynamic behaviour of benzodiazepines in reversed phase liquid chromatography. Chromatographia 1995, 41:84-87.
21. Hilgendorf C., Ahlin G., Seithel A., Artursson P., Ungell A.-L., Karlsson J. Expression of thirty-six drug transporters genes in human intestine, liver, kidney and organotypic cell lines. Drug Metab. Dispos. 2007, 35:1333-1340.
22. Hori Y., Fujisawa M., Shimada K., Hirose Y., Yoshioka T. Method for screening and quantitative determination of serum levels of salicylic acid, acetaminophen, theophylline, phenobarbital, bromvalerylurea, pentobarbital, and amobarbital using liquid chromatography/electrospray mass spectrometry. Biol. Pharm. Bull. 2006, 29(1):7-13.
23. Hosoja H., Kim K.J., Lee V.H.L. Age-dependent expression of P-glycoprotein gp170 in Caco-2 cell monolayers. Pharm. Res. 1996, 13:885-890.
24. Hu X.-Z., Xu Y., Yediler A. Determinations of residual furazolidone and its metabolite, 3-amino-2-oxazolidone (AOZ), in fish feeds by HPLC-UV and LC-MS/MS, respectively. J. Agric. Food Chem. 2007, 55:1144-1149.
25. Hummel D., Löffler D., Fink G., Ternes T.A. Simultaneous determination of psychoactive drugs and their metabolites in aqueous matrices by liquid chromatography mass spectrometry. Environ. Sci. Technol. 2006, 40(23):7321-7328.
26. Johnson R.D., Lewis R. Quantitation of atenolol, metoprolol, and propranolol in postmortem human fluid and tissue specimens via LC/APCI-MS. Forensic Sci. Int. 2006, 156:106-117.
27. Kansy M., Senner F., Gubernator K. Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes. J. Med. Chem. 1998, 41:1007-1010.
28. Kerns E.H., Di L., Petuski S., Farris M., Ley R., Jupp P. Combined application of parallel artificial membrane permeability assays in drug discovery. J. Pharm. Sci. 2004, 93:1440-1453.
29. Lang D., Böcker R. Highly sensitive and specific high-performance liquid chromatographic analysis of 7-hydroxywarfarin, a marker for human cytochrome P4502C9 activity. J. Chromatogr. B: Biomed. Sci. Appl. 1995, 672(2):305-309.
30. Lazorova L., Grasjo J., Bergstrom M., Wu F., Petterman-Bergstrom E., Ogren M., Langstrom B. Quantification and imaging of mannitol transport through Caco-2 cell monolayers using a positron-emitting tracer. Pharm. Res. 1998, 15(7):1141-1144.
31. Liang E., Chessic K., Yazdanian M. Evaluation of an accelerated Caco-2 cell permeability model. J. Pharm. Sci. 2000, 89(3):336-345.
32. Lu Q., Copper C.L., Collins G.E. Ultraviolet absorbance detection of colchicine and related alkaloids on a capillary electrophoresis microchip. Anal. Chim. Acta 2006, 572(2):205-211.
33. Matsson P., Bergstrom C.A.S., Nagahara N., Tavelin S., Norinder U., Artursson P. Exploring the role of different drug transport routes in permeability screening. J. Med. Chem. 2005, 48:604-613.
34. Maurer H.H., Tauvel F.X., Kraemer T. Screening procedure for detection of non-steroidal anti-inflammatory drugs and their metabolites in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons by gas chromatography-mass spectrometry after extractive methylation. J. Anal. Toxicol. 2001, 25(4):237-244.
35. Miraldi E., Masti A., Ferri S., Barni Comparini I. Distribution of hyoscyamine and scopolamine in Datura stramonium. Fitoterapia 2001, 72:644-648.
36. Miret S., Abrahamse L., De Groene E.M. Comparison of in vitro models for the prediction of compounds absorption across the human intestinal mucosa. J. Biomol. Screen. 2004, 9:598-606.
37. Niel E., Schermann J.M. Colchicine today. Joint Bone Spine 2006, 73:672-678.
38. Nigsch F., Klaffke W., Miret S. In vitro models for processes involved in intestinal absorption. Exp. Opin. Drug Metab. Toxicol. 2007, 34:545-556.
39. National Institute of Occupational Safety Health, 1994. Manual of Analytical Methods, 4th ed. Method 5512, Issue 2.
40. Oostendorp R.L., Beijnen J.H., Schellens J.H.M. The biological and clinical role of drug transporters at the intestinal barrier. Cancer Treat. Rev. 2009, 35:137-147.
41. Paine M.F., Hart H.L., Ludington S.S., Haining R.L., Rettie A.E., Zeldin D.C. The human intestinal cytochrome P450 "PIE" Drug Metab. Dispos. 2006, 34:880-886.
42. Palm K., Stenberg P., Luthman K., Artursson P. Polar molecular surface properties predict the intestinal absorption of drugs in humans. Pharm. Res. 1997, 14:568-571.
43. Pontier C., Pachot J., Botham R., Lenfant B., Arnaud P. HT29-MTX and Caco-2/TC7 monolayers as predictive models for human intestinal absorption: role of the mucus layer. J. Pharm. Sci. 2001, 90(10):1608-1619.
44. Pucci V., Monteagudo E., Bonelli F. High sensitivity determination of valproic acid in mouse plasma using semi-automated sample preparation and liquid chromatography with tandem mass spectrometric detection. Rapid Commun. Mass Spectrom. 2005, 19:3713-3718.
45. Rubas W., Cromwell M.E., Shahrokh Z., Villagran J., Nguyen T.N., Wellton M., Nguyen T.H., Mrsny R.J. Flux measurements across Caco-2 monolayers may predict transport in human large intestinal tissue. J. Pharm. Sci. 1996, 85:165-169.
46. Ryan T.W. Identification and quantification of tricyclic antidepressant by UV-photodiode array detection with multi-component analysis. J. Liquid Chromatogr. Relat. Technol. 1993, 16(7):1545-1560.
47. Seithel A., Karlsson J., Hilgendorf C., Björquist A., Ungell A.L. Variability in mRNA expression of ABC- and SLC-transporters in human intestinal cells: comparison between human segments and Caco-2 cells. Eur. J. Pharm. Sci. 2006, 28:291-299.
48. Selinger K., Lebel G., Hill H.M., Discenza C. High-performance liquid chromatographic method for the analysis of benztropine in human plasma. J. Chromatogr. 1989, 491(1):248-252.
49. Shin B.S., Yoon C.h., Balthasar J.P., Choi B.Y., Hong S.H., Kim H.J., Lee J.B., Hwang S.W., Yoo S.D. Prediction of drug availability in humans using immobilized artificial membrane phosphatidylcholine column chromatography and in vitro hepatic metabolic clearance. Biomed. Chromatogr. 2009, 23:764-769.
50. Surakitbanharn Y., McCandless R., Krzyzaniak J.F., Dannenfelser R.M., Yalkowsky S.H. Self-association of dexverapamil in aqueous solution. J. Pharm. Sci. 1995, 84(6):720-723.
51. Tambwekar K.R., Kakariya R.B., Garg S. A validated high performance liquid chromatographic method for analysis of nicotine in pure form and from formulations. J. Pharm. Biomed. Anal. 2003, 32(3):441-450.
52. Taur J.S., Rodriguez-Proteau R. Effects of dietary flavonoids on the transport of cimetidine via P-glycoprotein and cationic transporters in Caco-2 and LLC-PK1 cell models. Xenobiotica 2008, 38(12):1536-1550.
53. Thomas S., Brightman F., Gill H., Lee S., Pufong B. Simulation modelling of human intestinal absorption using Caco-2 permeability and kinetic solubility data for early drug discovery. J. Pharm. Sci. 2008, 97:4557-4574.
54. Tirelli V., Catone T., Turco L., Di Consiglio E., Testai E., De Angelis I. Effects of the pesticide chlorpyriphos on an in vitro model of intestinal barrier. Toxicol. In vitro 2007, 21:308-313.
55. Vachon P.H., Beaulieu J.F. Transient mosaic patterns of morphological and functional differentiation in the Caco-2 cell line. Gastroenterology 1992, 103:414-423.
56. Varma V.S.M., Kapoor N., Sarkar M., Panchagnula R. Simultaneous determination of digoxin and permeability markers in rat in situ intestinal perfusion samples by RP-HPLC. J. Chromatogr. B: Anal. Technol. Biomed. Life Sci. 2004, 813:347-352.
57. Verwei M., van de Berg H., Havenaar R., Groten J.P. Effect of folate-binding protein on intestinal transport of folic acid and 5-methyltetrahydrofolate across Caco-2 cells. Eur. J. Nutr. 2005, 44(4):242-249.
58. Walter E., Janich S., Roessler B.J., Amidon G., Hilfinger J.M., Amidon G.L. HT29-MTX/Caco-2 co-cultures as an in vitro model for the intestinal epithelium: in vitro-in vivo correlation with permeability data from rats and human. J. Pharm. Sci. 1996, 85(10):1070-1076.
59. Williams J.P., Nibbering N.M., Green B.N., Patel V.J., Scrivens J.H. Collision-induced fragmentation pathways including odd-electron ion formation from desorption electrospray ionisation generated protonated and deprotonated drugs derived from tandem accurate mass spectrometry. J. Mass Spectrom. 2006, 41(10):1277-1286.
60. Willmann S., Schmitt W., Keldenich J., Lippert J., Dressman J.B. A physiological model for the estimation of the fraction dose absorbed in humans. J. Med. Chem. 2004, 47:4022-4031.
61. Yamashita S., Furubayashi T., Kataoka M., Sakane T., Sezaki H., Tokuda H. Optimized conditions for prediction of intestinal drug permeability using Caco-2 cells. Eur. J. Pharm. Sci. 2000, 10:195-204.
62. Yee S. In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in man-fact or myth. Pharm. Res. 1997, 14(6):763-766.
63. Zhang L., Balimane P.V., Johnson S.R., Chong S. Development of an in silico model for predicting efflux substrates in Caco-2 cells. Int. J. Pharmacol. 2007, 343:98-105.
64. Zhao Y.H., Le J., Abraham M.H., Hersey A., Eddershaw P.J., Luscombe C.N., Boutina D., Beck G., Sherborne B., Cooper I., Platts J.A. Evaluation of human intestinal absorption data and subsequent derivation of a quantitative structure-activity relationship (QSAR) with the Abraham descriptors. J. Pharm. Sci. 2001, 90(6):749-784.
65. Zucco F., Batto A.F., Bises G., Chambaz J., Chiusolo A., Consalvo R., Cross H., Dal Negro G., De Angelis I., Fabre G., Guillou F., Hoffman S., Laplanche L., Morel E., Pinçon-Raymond M., Prieto P., Turco L., Ranaldi G., Rousset M., Sambuy Y., Scarino M.L., Torreilles F., Stammati A. An inter-laboratory study to evaluate the effects of medium composition on the differentiation and barrier function of Caco-2 cell lines. Altern. Lab. Animals 2005, 33(6):603-618.