Comparison of passive drug transport through Caco-2 cells and artificial membranes

International Journal of Pharmaceutics

Volumn 147, Issue 1, 1997, Pages 61-70

  Camenisch, Gian ^a,b   Folkers, Gerd ^b   Van De Waterbeemd, Han ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b ETH ZURICH   (Switzerland)

Author keywords

Artificial membranes; Caco 2 cell culture model; Diffusion cell; Passive diffusion; Permeability

Indexed keywords

ACTIVE TRANSPORT; ARTICLE; ARTIFICIAL MEMBRANE; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; CONTROLLED STUDY; DIFFUSION; DRUG TRANSPORT; HUMAN; HUMAN CELL; IN VITRO STUDY; LIPOPHILICITY; MOLECULAR WEIGHT; PARTITION COEFFICIENT; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; THEORY;

EID: 0030934676     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0378-5173(96)04796-5     Document Type: Article

References (43)

1. Albery, W.J., Burke, J.F., Leffler, E.B. and Hadgraft, J., Interfacial transfer studied with a rotating diffusion cell. J. Chem. Soc. Faraday Trans. 1, 72 (1976) 1618-1626.
2. Amidon, G.E., Higuchi, W.I. and Ho, N.F.H., Theoretical and experimental studies of transport of micelle-solubilized solutes. J. Pharm. Sci., 71 (1982) 77-84.
3. Arturrson, P., Cell culures as models for drug absorption across the intestinal mucosa. Crit. Rev. Ther. Drug Carrier Syst., 8 (1991) 305-330.
4. Artursson, P. and Karlsson, J., Correlation between oral drug absorption in humans and apparent permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem. Biophys. Res. Commun., 175 (1991) 880-885.
5. Camenisch, G., Folkers, G. and van de Waterbeemd, H., Review of passive drug absorption models: historical background, recent developments and limitations. Pharm. Acta Helv., (1996) (in press).
6. Conradi, R.A., Burton, P.S. and Borchard, R.T., Physicochemical and biological factors that influence a drug's cellular permeability by passive diffusion. In Pliska, V., Testa, B. and Van de Waterbeemd, H. (Eds.). Lipophilicity in Drug Action and Toxicology. VCH, Weinheim. 1996, pp. 233-252.
7. De Haan, F.H.N., De Vringer, T., Van de Waterbeemd, H. and Jansen, A.C.A., Transport in QSAR VII. Transport rate constants and transport rate parameters in various organic solvent-water systems. Int. J. Pharm., 13 (1983) 75-87.
8. De Haan, F.H.N. and Jangen, A.C.A., Development and application of model-based relationships describing in vivo absorption kinetics. In Seydel, J.K. (Ed.). QSAR and Strategies in the Design of Bioactive Compounds, VCH, Weinheim, 1985. pp. 198-204.
9. De Meere, A.L.J. and Tomlinson, E., Physicochemical description of the absorption rate of a drug through a membrane. Int. J. Pharm., 22 (1984) 177-196.
10. El Tayar, N., Tsai, R.S. and Carrupt, P.A., Polar intermolecular interactions encoded in partition coefficients: an indirect estimation of hydrogen-bonding parameters of polyfunctional solutes. J. Phys. Chem., 96 (1992) 1455-1459.
11. Fenstermacher, J.D., Blasberg, R.G. and Patlak, C.S., Methods for quantifying the transport of drugs across brain barrier systems. Pharmacol. Ther., 14 (1981) 217-248.
12. Flynn, G.L., Physicochemical determinants of skin absorption. In Gerrity, T.R. and Henry, C.J. (Eds). Principles of Route-to-Route Extrapolation for Risk Assessment, Elsevier, Amsterdam. 1990, pp. 93-127.
13. Flynn, G.L., Yalkowsky, S.H. and Roseman, T.J., Mass transport phenomena and models: theoretical concepts. J. Pharm. Sci., 63 (1974) 479-509.
14. Fujita, T., Iwasa, J. and Hansch, C., A new substituent constant. π, derived from partition coefficients. J. Am. Chem. Soc., 86 (1964) 5175-5180.
15. Gan, S., Eads, C., Niederer, T., Bridgers, A., Yanni, S., Hsyu, P.H., Pritchard, F.J. and Thakker, D., Use of Caco-2 as an in vitro intestinal absorption and metabolism model. Drug Dev. Ind. Pharm., 20 (1994) 615-631.
16. Hayton, W.L., Rate-limiting barriers to intestinal drug absorption: a review. J. Pharmacokinet. Biopharm., 8 (1980) 321-334
17. Hilgers, A.R., Conradi, R.A. and Burton, P.S., Caco-2 cell monolayers as a model for drug transport across the intestinal mucosa. Pharm. Res., 7 (1990) 902-910.
18. Hillgren, K.M., Kato, A. and Borchardt, R.T., In vitro systems for studying intestinal drug absorption. Med. Res. Rev., (1995) (in press).
19. Ho, N.F.H., Park, J.Y., Morozowich, W. and Higuchi, W.I., Physical model approach to the design of drugs with improved intestinal absorption. In Roche, E.B. (Ed.). Design of Biopharmaceutical Properties through Prodrugs and Analogs, APhA APS, Washington, DC, 1977, pp. 136-227.
20. Ho, N.F.H., Park, J.Y., Ni, P.F. and Higuchi, W.I., Advancing quantitative and mechanistic approaches in interfacing gastrointestinal drug absorption studies in animals and humans. In Crouthamel, W.G. and Sarapu, A. (Eds), Animal Models for Oral Drug Delivery in Man: In Situ and In Vivo Approaches, APhA APS, Washington, DC, 1983, pp. 27-106.
21. Hunter, J., Hirst, B.H. and Simmons, N.L., Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers. Pharm. Res., 10 (1993) 743-749.
22. Kamagami, S., Okabe, H., Kainose, H., Kikkawa, M. and Ishigami, Y., Penetration enhancement across a model membrane by liposomally entrapped drugs using N,N-diacylcysteine as a bilayer lipid. FEBS Lett., 281 (1991) 133-136.
23. Karlsson, J., Wikman, A. and Artursson, P., Transport of celiprolol across human intestinal epithelial (Caco-2) cells: medition of secretion by multiple transporters including P-glycoprotein. Br. J. Pharmacol., 110 (1993) 1009-1016.
24. Leahy, D.E., Lynch, J. and Taylor, D.C., Mechanims of absorption of small molecules. In Prescott, L.F. and Nimmo, W.S. (Eds.), Novel Drug Delivery and its Therapeutic Application, Wiley, New York, 1989, pp. 33-44.
25. Lennernäs, H., Does fluid flow across the intestinal mucosa affect quantitative oral drug absorption? Is it time for a reevaluation? Pharm. Res., 12 (1995) 1573-1582.
26. Levich, V.G., Convective diffusion in liquids. In Physicochemical Hydrodynamics. Prentice Hall, Englewood Cliffs, NJ, 1962.
27. Lieb, W.R. and Stein, W.D., The molecular basis of simple diffusion within biological membranes. Curr. Top. Membr. Transp., 2 (1971) 1-39.
28. Lippold, B.C. and Adel, M.S. Molekülassoziation in n-Octanol und n-Octanol-Wassergemischen. Arch. Pharm., 305 (1972) 417-426.
29. Noach, A.B.J., Enhancement of paracellular drug transport across epithelia in vitro and in vivo studies. PhD Thesis, University Leiden, 1994.
30. Rubas, W., Cromwell, M., Gadek, T., Narindray, D. and Mrsny, R., Structural elements which govern the resistance of intestinal tissues to compound transport. Mater. Res. Soc. Symp. Proc., 331 (1994) 179-185.
31. Schinkel, A.H., Wagenaar, E., Van Deemter, L., Mol., C.A.A. and Borst, P., Absence of the mdrla P-glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A. J. Clin. Invest., 96 (1995) 1698-1705.
32. Smith, R.N., Hansch, C. and Ames, M.M., Selection of a reference partitioning system for drug design work. J. Pharm. Sci., 64 (1975) 599-606.
33. Stehle, R.G. and Higuchi, W.I., In vitro model for transport of solutes in three-phase system. I. Theoretical principles. J Pharm. Sci., 61 (1972) 1922-1930.
34. Takanaga, H., Tamai, I. and Tsuji, A., pH-dependent and carrier-mediated transport of salicylic acid across Caco-2 cells. J. Pharm. Pharmacol., 46 (1994) 567-570.
35. Tamai, I., Takanaga, H., Maeda, H., Ogihara, T., Yoneda, M. and Tsuji, A., Proton-cotransport of pravastatin across intestianl brush-border membrane. Pharm. Res., 12 (1995) 1727-1732.
36. Tanaka, M., Fukuda, H. and Nagai, T., Permeation of drug through a model membrane consisting of millipore filter with oil. Chem. Pharm. Bull., 26 (1978) 9-13.
37. Tanaka, Y., Taki, Y., Sakane, T., Nadai, T., Sezaki, H. and Yamashita, S., Characterization of drug transport through tight-junctional pathway in Caco-2 monolayer: comparison with isolated rat jejunum and colon. Pharm. Res., 12 (1995) 523-528.
38. Testa, B. and Seiler, P., Steric and lipophilic components of the hydrophobic fragmental constant. Arzneim. Forsch. Drug Res., 31 (1981) 1053-1058.
39. Tsai, R.S., El Tayar, N., Carrupt, P.A. and Testa, B., Physicochemical properties and transport behaviour of piripidil: considerations on its membrane-crossing potential. Int. J. Pharm., 80 (1992) 39-49.
40. Van de Waterbeemd, H., The theoretical basis for relationships between drug transport and partition coefficients. In Dearden, J.C. (Ed.), Quantitative Approaches to Drug Design, Elsevier, Amsterdam, 1983, 183-192.
41. Walter, A. and Gutknecht, J., Permeability of small nonelectrolytes through lipid bilayer membranes. J. Membr. Biol., 90 (1986) 207-217.
42. Xiang, T.X. and Anderson, B.D., The relationship between permeant size and permeability in lipid bilayer membranes. J. Membr. Biol., 140 (1994) 111-122.
43. Yalkowsky, S.H., Slunick, T.G. and Flynn, G.L., Effects of alkyl chain length on biological activity: alkyl p-aminobenzoate-induced narcosis in goldfish. J. Pharm. Sci., 63 (1974) 691-695.