Excipients enhance intestinal absorption of ganciclovir by P-gp inhibition: Assessed in vitro by everted gut sac and in situ by improved intestinal perfusion

International Journal of Pharmaceutics

Volumn 403, Issue 1-2, 2011, Pages 37-45

  Li, Ming ^a   Si, Luqin ^a   Pan, Hongping ^a,b   Rabba, Abdullah K ^a   Yan, Fang ^a   Qiu, Jun ^a   Li, Gao ^a  

^a HUAZHONG UNIVERSITY OF SCIENCE AND TECHNOLOGY   (China)

^b PEOPLE'S HOSPITAL OF GUANGXI ZHUANG AUTONOMOUS REGION   (China)

Author keywords

BCS III drug; Everted gut sac; Excipient; P glycoprotein; Single pass intestinal perfusion

Indexed keywords

ACICLOVIR; CREMOPHOR; EXCIPIENT; GANCICLOVIR; GLYCOPROTEIN P; LACTATE DEHYDROGENASE; MACROGOL 400; POLOXAMER; POLYSORBATE 80; VERAPAMIL;

ANIMAL TISSUE; ARTICLE; BINDING SITE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG ADSORPTION; DRUG PENETRATION; DRUG STABILITY; ENZYME RELEASE; GLUCOSE TRANSPORT; INTESTINE MUCOSA PERMEABILITY; INTESTINE PERFUSION; MALE; MEMBRANE FLUIDITY; NONHUMAN; PRIORITY JOURNAL; RAT; SMALL INTESTINE ABSORPTION; WATER TRANSPORT;

ANIMALS; ANTIVIRAL AGENTS; BIOLOGICAL TRANSPORT; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; EPITHELIUM; EXCIPIENTS; GANCICLOVIR; GLUCOSE; INTESTINAL ABSORPTION; INTESTINE, SMALL; MALE; MODELS, BIOLOGICAL; P-GLYCOPROTEIN; PERFUSION; RATS; RATS, SPRAGUE-DAWLEY; SUBSTRATE SPECIFICITY;

EID: 78650177742     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2010.10.017     Document Type: Article

References (37)

1. E.K. Anderberg, C. Nystrom, and P. Artursson Epithelial transport of drugs in cell culture VII. Effects of pharmaceutical surfactant excipients and bile acids on transepithelial permeability in monolayers of human intestinal epithelial (Caco-2) cells J. Pharm. Sci. 81 1992 879 887
2. D.A. Ashiru, R. Patel, and A.W. Basit Polyethylene glycol 400 enhances the bioavailability of a BCS class III drug (Ranitidine) in male subjects but not females Pharm. Res. 25 2008 2327 2333
3. B.J. Aungst Intestinal permeation enhancers J. Pharm. Sci. 89 2000 429 442
4. M. Ballent, A. Lifschitz, G. Virkel, J. Sallovitz, and C. Lanusse Modulation of the P-glycoprotein-mediated intestinal secretion of ivermectin: in vitro and in vivo assessments Drug Metab. Dispos. 34 2006 457 463
5. T. Bansal, G. Mishra, M. Jaggi, R.K. Khar, and S. Talegaonkar Effect of P-glycoprotein inhibitor, verapamil, on oral bioavailability and pharmacokinetics of irinotecan in rats Eur. J. Pharm. Sci. 36 2009 580 590
6. L. Barthe, M. Bessouet, J.F. Woodley, and G. Houin The improved everted gut sac a simple method to study intestinal P-glycoprotein Int. J. Pharm. 173 1998 255 258
7. E.V. Batrakova, S. Li, Y. Li, V.Y. Alakhov, and A.V. Kabanov Effect of pluronic P85 on ATPase activity of drug efflux transporters Pharm. Res. 21 2004 2226 2233
8. E.V. Batrakova, S. Li, D.W. Miller, and A.V. Kabanov Pluronic P85 increases permeability of a broad spectrum of drugs in polarized BBMEC and Caco-2 cell monolayers Pharm. Res. 16 1999 1366 1372
9. J.R. Brown, J.H. Collett, D. Attwood, R.W. Ley, and E.E. Sims Influence of monocaprin on the permeability of a diacidic drug BTA-243 across Caco-2 cell monolayers and everted gut sacs Int. J. Pharm. 245 2002 133 142
10. T. Chang, L.Z. Benet, and M.F. Hebert The effect of water-soluble vitamin E on cyclosporine pharmacokinetics in healthy volunteers Clin. Pharmacol. Ther. 59 1996 297 303
11. W.L. Chiou, T.C. Wu, C. Ma, and H.Y. Jeong Enhanced oral bioavailability of decetaxel by coadministration of cyclosporine: quantitation and role of P-glycoprotein J. Clin. Oncol. 20 2002 1951 1952
12. T.J. Cook, and S.S. Shenoy Intestinal permeability of chlorpyrifos using a single-pass intestinal perfusion method in rat Toxicology 184 2003 125 133
13. P.K. Dudeja, K.M. Anderson, J.S. Harris, L. Buckingham, and J.S. Coon Reversal of multidrug resistance phenotype by surfactants: relationship to membrane fluidity Arch. Biochem. Biophys. 319 1995 309 315
14. C. Ehrhardt, and K.J. Kim Drug Absorption Studies In situ, In vitro and In silico Models 2008 Springer New York
15. J. Ferte Analysis of tangled relationships between P-glycoprotein- mediated multidrug resistance and the lipid phase of the cell membrane Eur. J. Biochem. 267 2001 277 294
16. B. Greiner, M. Eichelbaum, P. Fritz, H.P. Kreichgauer, O. von Richter, J. Zundler, and H.K. Kroemer The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin J. Clin. Invest. 104 1999 147 153
17. J.G. Huang, L.Q. Si, L.L. Jiang, Z.Z. Fan, J. Qiu, and G. Li Effect of pluronic F68 block copolymer on P-glycoprotein transport and CYP3A4 metabolism Int. J. Pharm. 356 2008 351 353
18. E.D. Hugger, K.L. Audus, and R.T. Brochard Effects of poly(elthyleneglycol) on efflux transporter activity in Caco-2 cell monolayers J. Pharm. Sci. 91 2002 1980 1990
19. E.D. Hugger, B.L. Novak, P.S. Burton, K.L. Audus, and R.T. Borchardt A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro J. Pharm. Sci. 91 2002 1991 2002
20. B.M. Johnson, W.N. Charman, and C.J. Porter An in vitro examination of the impact of polyethylene glycol 400, pluronic P85, and vitamin E d-a-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine AAPS PharmSci. 4 2002 E40
21. H. Lennernas Animal data: the contributions of the Ussing chamber and perfusion systems to predicting human oral drug delivery in vivo Adv. Drug Deliv. Rev. 59 2007 1103 1120
22. A. Loregian, R. Gatti, G. Palu, and E.F. De Palo Separation methods for acyclovir and related antiviral compounds J. Chromatogr. B 764 2001 289 311
23. B.D. Rege, J.P. Kao, and J.E. Polli Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers Eur. J. Pharm. Sci. 16 2002 237 246
24. R. Regev, Y.G. Assaraf, and G.D. Eytan Membrane fluidization by ether, other anesthetics, and certain agents abolishes P-glycoprotein ATPase activity and modulates efflux from multidrug-resistant cells Eur. J. Biochem. 259 1999 18 24
25. X.H. Ren, X.L. Mao, L. Cao, K.W. Xue, L.Q. Si, J. Qiu, A.D. Schimmer, and G. Li Nonionic surfactants are strong inhibitors of cytochrome P450 3A biotransformation activity in vitro and in vivo Eur. J. Pharm. Sci. 36 2009 401 411
26. M. Sababi, O. Borga, and U. Hultkvist-Bengtsson The role of P-glycoprotein in limiting intestinal regional absorption of digoxin in rats Eur. J. Pharm. Sci. 14 2001 21 27
27. E.C. Spoelstra, H.V. Westerhoff, H.M. Pinedo, H. Dekker, and J. Lankelma The multidrug-resistance-reverser verapamil interferes with cellular P-glycoprotein-mediated pumping of daunorubicin as a non-competing substrate Eur. J. Biochem. 221 1994 363 373
28. E.S. Swenson, W.B. Milisen, and W. Curatolo Intestinal permeability enhancement: efficacy, acute local toxicity, and reversibility Pharm. Res. 11 1994 1132 1142
29. T. Terao, E. Hisanaga, Y. Sai, I. Tamai, and A. Tsuji Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier J. Pharm. Pharmacol. 48 1996 1083 1089
30. R. Tian, N. Koyabu, H. Takanaga, H. Matsuo, H. Ohtani, and Y. Sawada Effects of grapefruit juice and orange juice on the intestinal efflux of P-glycoprotein substrates Pharm. Res. 19 2002 802 809
31. A.E. Trezise, P.R. Roman, D.R. Gill, S.C. Hyde, F.V. Sepulveda, M. Buchwald, and C.F. Higgins The multidrug resistance and cystic fibrosis genes have complementary patterns of epithelial expression EMBO J. 11 1992 4291 4303
32. K. Ueda, A. Yoshida, and T. Amachi Recent progress in P-glycoprotein research Anticancer Drug Des. 14 1999 115 121
33. M.V. Varma, Y. Ashokraj, C.S. Dey, and R. Panchagnula P-glycoprotein inhibitors and their screening: a perspective from bioavailability enhancement Pharmacol. Res. 48 2003 347 359
34. D. Wu, G. Li, J.G. Huang, Q. Chang, and X.G. Wu Study on relationship between the intestinal absorption of ganciclovir and the effect of drug efflux pump of P-gp China Pharm. 7 2004 408 411
35. Z. Yang, P. Manitpisitkul, and R.J. Sawchuk In situ studies of regional absorption of lobucavir and ganciclovir from rabbit intestine and predictions of dose-limited absorption and associated variability in humans J. Pharm. Sci. 95 2006 2276 2292
36. R. Yumoto, T. Murakami, Y. Nakamoto, R. Hasegawa, J. Nagai, and M. Takano Transport of rhodamine 123, a P-glycoprotein substrate, across rat intestine and Caco-2 cell monolayers in the presence of cytochrome P-450 3A-related compounds J. Pharmacol. Exp. Ther. 289 1999 149 155
37. H. Zhang, M. Yao, R.A. Morrison, and S. Chong Commonly used surfactant Tween 80, improves absorption of P-glycoprotein substrate, digoxin, in rats Arch. Pharm. Res. 26 2003 768 772