An in vitro examination of the impact of polyethylene glycol 400, Pluronic P85, and vitamin E d-α-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine

AAPS PharmSci

Volumn 4, Issue 4, 2002, Pages

  Johnson, Brendan M ^a   Charman, William N ^a   Porter, Christopher J H ^a  

^a MONASH UNIVERSITY   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATE; ALPHA TOCOPHEROL; BUFFER; CARRIER PROTEIN; CYTOCHROME P450 3A; DIGOXIN; EXCIPIENT; GLYCOPROTEIN P; GREPAFLOXACIN; KETOCONAZOLE; MIDAZOLAM; NORVERAPAMIL; POLOXAMER; PROTEINASE INHIBITOR; SOLUBILIZER; TALINOLOL; TOCOFERSOLAN; VALSPODAR; VERAPAMIL; MACROGOL DERIVATIVE; N DEMETHYLASE; SOLVENT; SUCCINIC ACID DERIVATIVE; UNSPECIFIC MONOOXYGENASE;

ANIMAL MODEL; ANIMAL TISSUE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DIFFUSION CHAMBER; DRUG METABOLISM; DRUG PENETRATION; DRUG TRANSPORT; IN VITRO STUDY; INTESTINE ABSORPTION; INTESTINE CELL; INTESTINE MUCOSA; JEJUNUM; MALE; MEMBRANE FLUIDITY; MITOCHONDRION; NONHUMAN; OSMOLARITY; RAT; REVIEW; SEROSA; ANIMAL; ARTICLE; CHEMISTRY; CYTOLOGY; DRUG EFFECT; INTESTINE; METABOLISM; SPRAGUE DAWLEY RAT; TRANSPORT AT THE CELLULAR LEVEL;

ADENOSINE TRIPHOSPHATE; ANIMALS; ARYL HYDROCARBON HYDROXYLASES; BIOLOGICAL TRANSPORT; CYTOCHROME P-450 CYP3A; DIGOXIN; ENTEROCYTES; INTESTINES; MALE; OXIDOREDUCTASES, N-DEMETHYLATING; P-GLYCOPROTEIN; POLOXAMER; POLYETHYLENE GLYCOLS; RATS; RATS, SPRAGUE-DAWLEY; SOLVENTS; SUCCINATES; VERAPAMIL; VITAMIN E;

EID: 0036453655     PISSN: 15221059     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (41)

1. 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;175:880-885.
2. Artursson P, Palm K, Luthman K. Caco-2 monolayers in experimental and theoretical predictions of drug transport. Adv Drug Deliv Rev. 2001;46:27-43.
3. Lennernas H, Nylander S, Ungell A-L. Jejunal permeability: a comparison between the Ussing chamber technique and the single-pass perfusion in humans. Pharm Res. 1997;14:667-671.
4. Thiebaut F, Tsuruo T, Hamada H, Gottesman MM, Pastan I, Willingham MC. Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues. Proc Natl Acad Sci U S A. 1987;84:7735-7738.
5. Greiner B, Eichelbaum M, Fritz P, et al. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J Clin Invest. 1999;104:147-153.
6. Kim AE, Dintaman JM, Waddell DS, Silverman JA. Saquinavir, an HIV protease inhibitor, is transported by P-glycoprotein. J Pharmacol Exp Ther. 1998;286:1439-1445.
7. Yamaguchi H, Yano I, Saito H, Inui KI. Pharmacokinetic role of P-glycoprotein in oral bioavailability and intestinal secretion of grepafloxacin in vivo. J Pharmacol Exp Ther. 2002;300:1063-1069.
8. Spahn-Langguth H, Baktir G, Radschuweit A, et al. P-glycoprotein transporters and the gastrointestinal tract: evaluation of the potential in vivo relevance of in vitro data employing talinolol as a model compound. Int J Clin Pharmacol Ther. 1998;36:16-24.
9. de Waziers I, Cugnenc PH, Yang CS, Leroux J-P, Beaune PH. Cytochrome P450 isoenzymes, epoxide hydrolase and glutathione transferases in rat and human hepatic and extrahepatic tissues. J Pharmacol Exp Ther. 1990;253:387-394.
10. von Richter O, Greiner B, Fromm MF, et al. Determination of in vivo absorption, metabolism, and transport of drugs by the human intestinal wall and liver with a novel perfusion technique. Clin Pharmacol Ther. 2001;70:217-227.
11. Gomez DY, Wacher VJ, Tomlanovich SJ, Hebert MF, Benet LZ. The effects of ketoconazole on the intestinal metabolism and bioavailability of cyclosporine. Clin Pharmacol Ther. 1995;58:15-19.
12. Lown KS, Bailey DG, Fontana RJ, et al. Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. J Clin Invest. 1997;99:2545-2553.
13. Cummins CL, Jacobsen W, Benet LZ. Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4. J Pharmacol Exp Ther. 2002;300:1036-1045.
14. Gottesman MM, Pastan I. Biochemistry of multidrug resistance mediated by the multidrug transporter. Annu Rev Biochem. 1993;62:385-427.
15. Nerurkar MM, Burton PS, Borchardt RT. The use of surfactants to enhance the permeability of peptides through Caco-2 cells by inhibition of an apically polarized efflux system. Pharm Res. 1996;13:528-534.
16. Mountfield RJ, Senepin S, Schleimer M, Walter I, Bittner B. Potential inhibitory effects of formulation ingredients on intestinal cytochrome P450. Int J Pharm. 2000;211:89-92.
17. Anderle P, Niederer E, Rubas W, et al. P-glycoprotein (P-gp) mediated efflux in Caco-2 cell monolayers: the influence of culturing conditions and drug exposure on P-gp expression levels. J Pharm Sci. 1998;87:757-762.
18. Fojo AT, Ueda K, Slamon DJ, Poplack DG, Gottesman MM, Pastan I. Expression of a multidrug-resistance gene in human tumors and tissues. Proc Natl Acad Sci U S A. 1987;84:265-269.
19. Prueksaritanont T, Gorham LM, Hochman JH, Tran LO, Vyas KP. Comparative studies of drug-metabolizing enzymes in dog, monkey, and human small intestines, and in Caco-2 cells. Drug Metab Dispos. 1996;24:634-642.
20. Taipalensuu J, Tornblom H, Lindberg G, et al. Correlation of gene expression of ten drug efflux proteins of the ATP-binding cassette transporter family in normal human jejunum and in human intestinal epithelial Caco-2 cell monolayers. J Pharmacol Exp Ther. 2001;299:164-170.
21. Batrakova EV, Miller DW, Li S, Alakhov VY, Kabanov AV, Elmquist WF. Pluronic P85 enhances the delivery of digoxin to the brain: in vitro and in vivo studies. J Pharmacol Exp Ther. 2001;296:551-557.
22. Yu L, Bridgers A, Polli J, et al. Vitamin E-TPGS increases absorption flux of an HIV protease inhibitor by enhancing its solubility and permeability. Pharm Res. 1999;16:1812-1817.
23. Wacher VJ, Wu CY, Benet LZ. Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy. Mol Carcinog. 1995;13:129-134.
24. Johnson BM, Charman WN, Porter CJH. The impact of P-glycoprotein efflux on enterocyte residence time and enterocyte-based metabolism of verapamil. J Pharm Pharmacol. 2001;53:1611-1619.
25. Saitoh H, Aungst BJ. Possible involvement of multiple P-glycoprotein-mediated efflux systems in the transport of verapamil and other organic cations across rat intestine. Pharm Res. 1995;12:1304-1310.
26. Batrakova EV, Han HY, Alakhov VY, Miller DW, Kabanov AV. Effects of pluronic block copolymers on drug absorption in Caco-2 cell monolayers. Pharm Res. 1998;15:850-855.
27. Nyberg L, Bratt L, Forsgren A, Hugosson S. Bioavailability of digoxin from tablets, I: in vitro characterization of digoxin tablets. Acta Pharm Suec. 1974;11:447-458.
28. Petersen R, Flasch H, Heinz N. Darstellung und eigenschaften einiger glukuronide und sulfate von cardenoliden und cardenolid-glykosiden. Arzneimittelforschung. 1977;27:642-649.
29. Litman T, Druley TE, Stein WD, Bates SE. From MDR to MXR: new understanding of multidrug resistance systems, their properties and clinical significance. Cell Mol Life Sci. 2001;58:931-959.
30. Tang F, Horie K, Borchardt RT. Are MDCK cells transfected with the human MRP2 gene a good model of the intestinal mucosa? J Pharm Sci. 2002;19:773-779.
31. Stephens RH, O'Neill CA, Warhurst A, Carlson GL, Rowland M, Warhurst G. Kinetic profiling of P-glycoprotein-mediated drug efflux in rat and human intestinal epithelia. J Pharmacol Exp Ther. 2001;296:584-591.
32. Kroemer HK, Gautier J-C, Beaune P, Henderson C, Wolf CR, Eichelbaum M. Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993;348:332-337.
33. Batrakova EV, Han HY, Miller DW, Kabanov AV. Effects of pluronic P85 unimers and micelles on drug permeability in polarized BBMEC and Caco-2 cells. Pharm Res. 1998;15:1525-1532.
34. Pauli-Magnus C, von Richter O, Burk O, et al. Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein. J Pharmacol Exp Ther. 2000;293:376-382.
35. Batrakova EV, Li S, Vinogradov SV, Alakhov VY, Miller DW, Kabanov AV. Mechanism of Pluronic effect on P-glycoprotein efflux system in blood-brain barrier: contributions of energy depletion and membrane fluidization. J Pharmacol Exp Ther. 2001;299:483-493.
36. Batrakova EV, Li S, Alakhov VY, Kabanov AV. Selective energy depletion and sensitization of multiple drug resistant cancer cells by Pluronic block copolymers. Polym Prepr. 2000;41:1639-1640.
37. Rapoport N, Marin AP, Timoshin AA. Effect of a polymeric surfactant on electron transport in HL-60 cells. Arch Biochem Biophys. 2000;384:100-108.
38. Regev R, Assaraf YG, Eytan GD. Membrane fluidization by ether, other anesthetics, and certain agents abolishes P-glycoprotein ATPase activity and modulates efflux from multidrug-resistant cells. Eur J Biochem. 1999;259:18-24.
39. Dudeja PK, Anderson KM, Harris JS, Buckingham L, Coon JS. Reversal of multidrug resistance phenotype by surfactants: relationship to membrane fluidity. Arch Biochem Biophys. 1995;319:309-315.
40. Callaghan R, Stafford A, Epand RM. Increased accumulation of drugs in a multidrug resistant cell line by alteration of membrane biophysical properties. Biochim Biophys Acta. 1993;1175:277-282.
41. Krugliak P, Hollander D, Schlaepfer CC, Nguyen H, Ma TY. Mechanisms and sites of mannitol permeability of small and large intestine in the rat. Dig Dis Sci. 1994;39:796-801.