Functional role of P-glycoprotein in limiting intestinal absorption of drugs: Contribution of passive permeability to P-glycoprotein mediated efflux transport

Molecular Pharmaceutics

Volumn 2, Issue 1, 2005, Pages 12-21

  Varma, Manthena V S ^a   Sateesh, Khandavilli ^a   Panchagnula, Ramesh ^a  

^a NATIONAL INSTITUTE OF PHARMACEUTICAL EDUCATION AND RESEARCH NIPER   (India)

Author keywords

Absorption quotient; Biopharmaceutics Classification System; Intestinal permeability; Lipinski's rule of 5; P glycoprotein

Indexed keywords

ADENOSINE TRIPHOSPHATASE; ALPRENOLOL; AMANTADINE; AMITRIPTYLINE; ATENOLOL; BIPERIDEN; BROMOCRIPTINE; BUFURALOL; BUSPIRONE; CARBAMAZEPINE; CHLORPHENIRAMINE; CHLORPROTHIXENE; CLEMASTINE FUMARATE; CLOMIPRAMINE; CLONIDINE; CYCLOBENZAPRINE; DESIPRAMINE; DIPHENHYDRAMINE; DOXAPRAM; DOXEPIN; DOXORUBICIN; DOXYLAMINE; ELACRIDAR; FLUMAZENIL; FLUOXETINE; FLURAZEPAM; FLUVOXAMINE; GLYCOPROTEIN P; PHENAZONE; UNINDEXED DRUG;

ANIMAL CELL; ARTICLE; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG SOLUBILITY; ENZYME ACTIVITY; HUMAN; HYDROGEN BOND; INTESTINE ABSORPTION; INTESTINE MUCOSA PERMEABILITY; MOLECULAR WEIGHT; NONHUMAN; PASSIVE TRANSPORT; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; SURFACE PROPERTY;

ADENOSINE TRIPHOSPHATASES; ANIMALS; BIOLOGICAL AVAILABILITY; BIOLOGICAL TRANSPORT; CELL LINE; CELL MEMBRANE PERMEABILITY; DOGS; FLUORESCEINS; HUMANS; INTESTINAL ABSORPTION; P-GLYCOPROTEIN; P-GLYCOPROTEINS; PHARMACEUTICAL PREPARATIONS; PREDICTIVE VALUE OF TESTS; SOLUBILITY;

EID: 14644419054     PISSN: 15438384     EISSN: None     Source Type: Journal    
DOI: 10.1021/mp0499196     Document Type: Article

References (35)

1. Amidon, G. L.; Lennernas, H.; Shah, V. P.; Crison, J. R. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 1995, 12, 413-420.
2. Varma, M. V. S.; Ashokraj, Y.; Dey, C. S.; Panchagnula, R. P-glycoprotein inhibitors and their screening: a perspective from bioavailability enhancement. Pharmacol Res. 2003, 48, 347-359.
3. Ambudkar, S. V.; Dey, S.; Hrycyna, C. A.; Ramchandra, M.; Pastan, I.; Gottesman, M. M. Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annu. Rev. Pharmacol. Toxicol. 1999, 39, 361-398.
4. Williams, W. C.; Sinko, P. J. Oral absorption of the HIV protease inhibitors: a current update. Adv. Drug Del. Rev. 1999, 39, 211-238.
5. Chiou, W. L.; Chung, S. M.; Wu, T. C. Apparent lack of effect of P-glycoprotein on the gastrointestinal absorption of a substrate, tacrolimus, in normal mice. Pharm. Res. 2000, 17, 205-208.
6. Chiou, W. L.; Chung, S. M.; Wu, T. C.; Ma, C. A comprehensive account on the role of efflux transporters in the gastrointestinal absorption of 13 commonly used substrate drugs in humans. Int. J. Clin. Pharmacol. Ther. 2001, 39, 93-101.
7. Chiou, W. L.; Ma, C.; Chung, S. M.; Wu, T. C. An alternative hypothesis to involvement of intestinal P-glycoprotein as the cause for digoxin oral bioavailability enhancement by talinolol. Clin. Pharmacol. Ther. 2001, 69, 79-81.
8. Woo, J. S.; Lee, C. H.; Shim, C. K.; Hwang, S. J. Enhanced oral bioavailability of paclitaxel by coadministration of the P-glycoprotein inhibitor KR30031. Pharm. Res. 2003, 20, 24-30.
9. Spahn-Langguth, H.; Baktir, G.; Radschuweit, A.; Okyar, A.; Terhaag, B.; Ader, P.; Hanafy, A.; Langguth, P, P-glycoprotein transporters and the gastrointestinal tract: evaluation of the potential in vivo relevance of in vitro data employing talinolol as model compound. Int. J. Clin. Pharmacol. Ther. 1998, 36, 16-24.
10. Schwarz, U. I.; Gramatte, T.; Krappweis, J.; Oertel, R.; Kirch, W. P-glycoprotein inhibitor erythromycin increases oral bioavailability of talinolol in humans. Int. J. Clin. Pharmacol. Ther. 2000, 38, 161-167.
11. Meaden, E. R.; Hoggard, P. G.; Newton, P.; Tjia, J. F.; Aldam, D.; Cornforth, D.; Lloyd, J.; Williams, I.; Back, D. J.; Khoo, S. H. P-glycoprotein and MRP1 expression and reduced ritonavir and saquinavir accumulation in HIV-infected individuals. J. Antimicrob. Chemother. 2002, 50, 583-588.
12. Polli, J. W.; Wring, S. A.; Humphreys, J. E.; Huang, L.; Morgan, J. B.; Webster, L. O.; Serabjit-Singh, C. S. Rational use of in vitro P-glycoprotein assays in drug discovery. J. Pharmacol. Exp. Ther. 2001, 299, 620-628.
13. Mahar Doan, K. M.; Humphreys, J. E.; Webster, L. O.; Wring, S. A.; Shampine, L. J.; Serabjit-Singh, C. J.; Adkison, K. K.; Polli, J. W. Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J. Pharmacol. Exp. Ther. 2002, 303, 1029-1037.
14. Physicians' Desk Reference, 57th ed.; Thomson, PDR: Montvale, NJ, 2003.
15. USP DI Volume III, Approved drug products and legal requirements, 18th ed.; United States Pharmacopeial Convention, Inc.: Rockville, MD, 1998.
16. Therapeutic drugs, 2nd ed.; Churchill Livingstone: Edinburgh, U.K., 1999.
17. Zhao, Y. H.; Le, J.; Abraham, M. H.; Hersey, A.; Eddershaw, P. J.; Luscombe, C. N.; Butina, D.; Beck, G.; Sherborne, B.; Cooper, I.; Platts, J. A.; Boutina, D. 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, 749-784.
18. The United States Pharmacopeia, 24th ed.; United States Pharmacopeial Convention, Inc.; Philadelphia, PA, 2000.
19. The Merck Index, 13th ed.; Merck Research laboratories: Rahway, NJ, 2001.
20. Irvine, J. D.; Takahashi, L.; Lockhark, K.; Cheong, I.; Tolan, J. W.; Selick, H. E.; Grove, J. R. MDCK (Madin-Darby canine kidney) cells: a tool for membrane permeability screening. J. Pharm. Sci. 1999, 88, 28-33.
21. Tang, F.; Horie, K.; Borchardt, R. T. Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa? Pharm. Res. 2002, 19, 765-772.
22. Tang, F.; Borchardt, R. T. Characterization of the efflux transporter(s) responsible for restricting intestinal mucosa permeation of the coumarinic acid-based cyclic prodrug of the opioid peptide DADLE. Pharm. Res. 2002, 19, 787-793.
23. Tang, F.; Borchardt, R. T. Characterization of the efflux transporter(s) responsible for restricting intestinal mucosa permeation of an acyloxyalkoxy-based cyclic prodrug of the opioid peptide DADLE. Pharm. Res. 2002, 19, 780-786.
24. Lentz, K. A.; Polli, J. W.; Wring, S. A.; Humphreys, J. E.; Polli, J. E. Influence of passive permeability on apparent P-glycoprotein kinetics. Pharm. Res. 2000, 17, 1456-1460.
25. Doppenschmitt, S.; Spahn-Langguth, H.; Regardh, C. G,; Langguth, P. Role of P-glycoprotein-mediated secretion in absorptive drug permeability: An approach using passive membrane permeability and affinity to P-glycoprotein. J. Pharm. Sci. 1999, 88, 1067-1072.
26. Troutman, M. D.; Thakker, D. R. Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharm. Res. 2003, 20, 1210-1224.
27. Lipinski, C. A.; Lombarde, F.; Dominy, B. W.; Feeney, P. J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Delivery Rev. 2001, 46, 3-26.
28. Kasim, N. A.; Whitehouse, M.; Ramachandran, C.; Bermejo, M.; Lennernäs, H.; Hussain, A. S.; Junginger, H. E.; Stavchansky, S. A.; Midha, K. K.; Shah, V. P.; Amidon, G. L. Molecular properties of WHO essential drugs and provisional biopharmaceutical classification. Mol. Pharm. 2004, 1, 85-96.
29. 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.
30. Yu, L. X.; Amidon, G. L.; Polli, J. E.; Zhao, H.; Mehta, M. U.; Conner, D. L.; Hussain, A. S. Biopharmaceutics classification system: the scientific basis for biowaiver extensions. Pharm. Res. 2002, 19, 921-925.
31. Rinaki, E.; Valsami, G.; Macheras, P. Quantitative biopharmaceutics classification system: the central role of dose/solubility ratio. Pharm. Res. 2003, 20, 1917-1925.
32. Varma, M. V. S.; Sateesh, K.; Ashokraj, Y.; Jain, A.; Dhanikula, A.; Sood, A.; Thomas, N. S.; Pillai, O.; Sharma, P.; Gandhi, R.; Agrawal, S.; Nair, V.; Panchagnula, R. Biopharmaceutic classification system: A scientific framework for pharmacokinetic optimization in drug research. Curr. Drug Metab. 2003, 5, 375-388.
33. Paine, M. F.; Shen, D. D.; Kunze, K. L.; Perkins, J. D.; Marsh, C. L.; McVicar, J. P.; Barr, D. M.; Gillies, B. S.; Thummel, K. E. First-pass metabolism of midazolam by the human intestine. Clin. Pharmacol. Ther. 1996, 60, 14-24.
34. Mouly, S.; Paine, M. F. P-glycoprotein increases from proximal to distal regions of human small intestine. Pharm. Res. 2003, 20, 1595-1599.
35. Siegmund, W.; Ludwig, K.; Engel, G.; Zschiesche, M.; Franke, G.; Hoffmann, A.; Terhaag, B.; Weitschies, W. Variability of intestinal expression of P-glycoprotein in healthy volunteers as described by absorption of talinolol from four bioequivalent tablets. J. Pharm. Sci. 2003, 92, 604-610.