Effects of poly(ethylene glycol) on efflux transporter activity in Caco-2 cell monolayers

Journal of Pharmaceutical Sciences

Volumn 91, Issue 9, 2002, Pages 1980-1990

  Hugger, Erin D ^a,b   Audus, Kenneth L ^a   Borchardt, Ronald T ^a  

^a UNIVERSITY OF KANSAS   (United States)

^b GLAXOSMITHKLINE   (United States)

Author keywords

Caco 2 cells; Cell membrane fluidity; P glycoprotein; Poly(ethylene glycol) (PEG)

Indexed keywords

ANTINEOPLASTIC AGENT; CARBON 14; CHOLESTEROL; DOXORUBICIN; EXCIPIENT; GLYCOPROTEIN P; MACROGOL; MANNITOL; MULTIDRUG RESISTANCE PROTEIN; PACLITAXEL; TESTOSTERONE; TRITIUM;

ARTICLE; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; DRUG FORMULATION; DRUG PENETRATION; HUMAN; HUMAN CELL; INTESTINE MUCOSA; INTESTINE MUCOSA PERMEABILITY; MEMBRANE FLUIDITY; MONOLAYER CULTURE;

EID: 0036771089     PISSN: 00223549     EISSN: None     Source Type: Journal    
DOI: 10.1002/jps.10175     Document Type: Article

References (38)

1. Pauletti GM, Gangwar S, Knipp GT, Nerurkar MM, Okumu FW, Tamura K, Siahaan TJ, Borchardt RT. 1996. Structural requirements for the intestinal absorption of peptide drugs. J Controlled Release 41:3-17.
2. Conradi RA, Burton PS, Borchardt RT. 1996. Physicochemical and biological factors that influence a drug's cellular permeability by passive diffusion. In: Pliska V, Testa B, van de Waterbeemd H, Mannhold R, Kubinyi H, Timmerman H, editors. Drug action and toxicology. New York: VCH Publishers. pp. 233-252.
3. Gangwar S, Pauletti GM, Wang B, Siahaan TJ, Stella VJ, Borchardt RT. 1997. Prodrug strategies to enhance intestinal absorption of peptides. Drug Discov Today 2:148-155.
4. Benet LZ, Wu C, Hebert MF, Wacher VJ. 1996. Intestinal drug metabolism and antitransport processes: a potential paradigm shift in oral drug delivery. J Controlled Release 39:139-143.
5. Watkins PB. 1997. The barrier function of CYP3A4 and P-glycoprotein in the small bowel. Adv Drug Deliv Rev 27:235-256.
6. Ambudkar SV, Dey S, Hrycyna A, Ramachandra M, Pastan I, Gottesman MM. 1999. Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Ann Rev Pharmacol Toxicol 39:361-398.
7. Cordon-Cardo C, O'Brien JP, Boccia J, Casals D, Bertino JR, Melamed MR. 1990. Expression of the multidrug resistance gene product (P-glycoprotein) in human normal and tumor tissues. J Histochem Cytochem 38:1277-1287.
8. Gupta S. 1995. P-glycoprotein expression and regulation. Drugs Aging 7:19-29.
9. 4 and structurally related conjugates. J Biol Chem 269:27807-27810.
10. Gutmann H, Fricker G, Török M, Michael S, Beglinger C, Drewe J. 1999. Evidence for different ABC-transporters in Caco-2 cells modulating drug uptake. Pharm Res 16:402-407.
11. Hunter JM, Jepson A, Tsuro T, Simmons NL, Hirst BH. 1993. Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells. J Biol Chem 268:14991-14997.
12. Krishna R, Mayer LD. 2000. Multidrug resistance (MDR) in cancer mechanisms, reversal using modulators of MDR and the role of MDR in influencing the pharmacokinetics of anticancer drugs. Eur J Pharm Sci 11:265-283.
13. van Asperen J, van Tellingen O, Sparreboom A, Schinkel AH, Borst P, Nooijen WJ, Beijen JH. 1997. Enhanced oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833, Br J Cancer 76:1181-1183.
14. van Asperen J, van Tellingen O, van der Walk MA, Rozenhart M, Beijen JH. 1998. Enhanced oral absorption and decreased elimination of paclitaxel in mice cotreated with cyclosporin A. Clin Cancer Res 4:2293-2297.
15. Hyafil F, Vergely C, Du Vignaud P, Grand-Perret T. 1993. In vitro and in vivo reversal of multidrug resistance by GF 120918, an acridonecarboxamide derivative. Cancer Res 53:4595-4602.
16. Woodcock DM, Jefferson S, Linsenmeyer ME, Crowther PJ, Chojnowski GM, Williams B, Bertoncello I. 1990. Reversal of the multidrug resistance phenotype with Cremophor EL, a common vehicle for water-insoluble vitamins and drug. Cancer Res 50:4199-4203.
17. Woodcock DM, Linsenmeyer ME, Chojnowski G, Kriegler AB, Nink V, Webster LK, Sawyer WH. 1992. Reversal of multidrug resistance by surfactants. Br J Cancer 66:62-68.
18. Zordan-Nudo T, Ling V, Liu Z, Georges E. 1993. Effects of nonionic detergents on P-glycoprotein drug binding and reversal of multidrug resistance. Cancer Res 53:5994-6000.
19. Nerurkar MM, Ho NFH, Burton PS, Borchardt RT. 1996. The use of surfactants to enhance the permeability of peptides through Caco-2 cells by inhibition of an apically polarized efflux mechanism. Pharm Res 13:528-534.
20. Nerurkar MM, Ho NFH, Burton PS, Vidmar TJ, Borchardt RT. 1997. Mechanistic roles of neutral surfactants on concurrent polarized and passive membrane transport of a model peptide in Caco-2 cells. J Pharm Sci 86:813-821.
21. Artursson P, Palm K, Luthman K. 1996. Caco-2 cell monolayers in experimental and theoretical predictions of drug transport. Adv Drug Deliv Rev 22:67-84.
22. Hidalgo IJ, Raub TJ, Borchardt RT. 1989. Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology 96:736- 749.
23. Burton PS, Conradi RA, Hilgers AR, Ho NFH. 1993. Evidence for a polarized efflux system for peptides in the apical membrane of Caco-2 cells. Biochem Biophys Res Comm 190:760-766.
24. Price JC. 1994. Polyethylene glycol. In: Wade A, Weller PJ, editors. Handbook of pharmaceutical excipients, 2nd ed. London: The Pharmaceutical Press; pp. 355-361.
25. Dudeja PK, Anderson KM, Harris JS, Buckingham L, Coon JS. 1995. Reversal of multidrug resistance related phenotype by surfactants: relationship to membrane fluidity. Arch Biochem Biophys 319:309-315.
26. Hugger ED, Novak BL, Burton PS, Audus KL, Borchardt RT. A comparision of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. J Pharm Sci 91:1991-2002.
27. Gao J, Hugger ED, Beck-Westermeyer MS, Borchardt RT. 2000. Estimating intestinal mucosal permeation of drugs using Caco-2 cell monolayers. In: Enna SJ, Williams M, Ferkany JW, Kenakin T, Porsolt RE, Sullivan JP, editors. Current protocols in pharmacology. New York: John Wiley & Sons; Unit 7.2. pp. 1-23.
28. Walle UK, Walle T. 1998. Taxol transport by human intestinal epithelial Caco-2 cells. Drug Metab Dispos 26:343-346.
29. Flynn GL, Yalkowsky SH, Roseman TJ. 1974. Mass transport phenomena and models: theoretical concepts. J Pharm Sci 63:479-510.
30. Ho NFH, Burton PS, Conradi RA, Barsuhn CL. 1995. A biophysical model of passive and polarized active transport processes in Caco-2 cells: approaches to uncoupling apical and basolateral membrane events in the intact cell. J Pharm Sci 84:21-27.
31. Audus KL, Guillot FL, Braughler JM. 1991. Evidence for 21-aminosteroid association with the hydrophobic domains of brain microvessel endothelial cells. Free Radic Biol Med 11:361-371.
32. Gudmundsson OS, Pauletti GM, Wang W, Shan D, Zhang H, Wang B, Borchardt RT. 1999. Coumarinic acid-based cyclic prodrugs of opioid peptides that exhibit metabolic stability to peptidases and excellent cellular permeability. Pharm Res 16:7-15.
33. Hilgers AR, Conradi RA, Burton PS. 1990. Caco-2 cell monolayers as a model for drug transport in the intestinal mucosa. Pharm Res 7:902-910.
34. Donegan L, Hudye SA, Hardin JA, Gall DG. 1999. Effect of a dietary nonionic surfactant on small intestinal nutrient transport. Digest Dis Sci 44:1423-1427.
35. Schreier S, Malheiros SVP, de Paula E. 2000. Surface active drugs: self-association and interaction with membranes and surfactants. Physicochemical and biological aspects. Biochim Biophys Acta 1508:210-234.
36. Yalkowsky SH. 1999. Solubilization by surfactants. In: Solubility and solubilization in aqueous media. New York: Oxford University Press; pp. 236-320.
37. Nooter K, Oostrum R, Deurloo J. 1987. Effects of verapamil on the pharmacokinetics of daunomycin in the rat. Cancer Chemother Pharmacol 20:176-178.
38. Ferté J. 2000. Analysis of tangled relationships between P-glycoprotein-mediated multidrug resistance and the lipid phase of the cell membrane. Eur J Biochem 267:277-294.