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Intestinal transporters: enhanced absorption through P-glycoprotein-related drug interactions

& (Professor of Pharmaceutics)

Bibliography

  • Barta CA, Sachs-Barrable K, Feng F, Wasan KM. Effects of monoglycerides on P-glycoprotein: modulation of the activity and expression in Caco-2 cell monolayers. Mol Pharm 2008;5(5):863-75
  • Song NN, Zhang SY, Liu CX. Overview of factors affecting oral drug absorption. Asian J Drug Metab Pharmacokinet 2004;4(3):167-76
  • Steffansen B, Nielsen CU, Brodin B, et al. Intestinal solute carriers: an overview of trends and strategies for improving oral drug absorption. Eur J Pharm Sci 2004;21(1):3-16
  • Lee VH. Membrane transporters. Eur J Pharm Sci 2000;11(Suppl 2):S41-50
  • Hagenbuch B, Meier PJ. Organic anion transporting polypeptides of the OATP/SLC21 family: phylogenetic classification as OATP/SLCO superfamily, new nomenclature and molecular/functional properties. Pflügers Arch 2004;447(5):653-65
  • Kobayashi D, Nozawa T, Imai K, et al. Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH-dependent transport across intestinal apical membrane. J Pharmacol Exp Ther 2003;306(2):703-8
  • Grandvuinet AS, Vestergaard HT, Rapin N, Steffansen B. Intestinal transporters for endogenic and pharmaceutical organic anions: the challenges of deriving in-vitro kinetic parameters for the prediction of clinically relevant drug-drug interactions. J Pharm Pharmacol 2012;64(11):1523-48
  • Sai Y, Tsuji A. Transporter-mediated drug delivery: recent progress and experimental approaches. Drug Discov Today 2004;9(16):712-20
  • Koepsell H. Polyspecific organic cation transporters: their functions and interactions with drugs. Trends Pharmacol Sci 2004;25(7):375-81
  • Hagenbuch B, Meier PJ. The superfamily of organic anion transporting polypeptides. Biochim Biophys Acta 2003;1609(1):1-18
  • Tapaninen T, Neuvonen PJ, Niemi M. Grapefruit juice greatly reduces the plasma concentrations of the OATP2B1 and CYP3A4 substrate aliskiren. Clin Pharmacol Ther 2010;88(3):339-42
  • Dresser GK, Kim RB, Bailey DG. Effect of grapefruit juice volume on the reduction of fexofenadine bioavailability: possible role of organic anion transporting polypeptides. Clin Pharmacol Ther 2005;77(3):170-7
  • Imanaga J, Kotegawa T, Imai H, et al. The effects of the SLCO2B1 c.1457C > T polymorphism and apple juice on the pharmacokinetics of fexofenadine and midazolam in humans. Pharmacogenet Genomics 2011;21(2):84-93
  • Lilja JJ, Juntti-Patinen L, Neuvonen PJ. Orange juice substantially reduces the bioavailability of the beta-adrenergic-blocking agent celiprolol. Clin Pharmacol Ther 2004;75(3):184-90
  • Lilja JJ, Raaska K, Neuvonen PJ. Effects of orange juice on the pharmacokinetics of atenolol. Eur J Clin Pharmacol 2005;61(5-6):337-40
  • Schwarz UI, Seemann D, Oertel R, et al. Grapefruit juice ingestion significantly reduces talinolol bioavailability. Clin Pharmacol Ther 2005;77(4):291-301
  • Neuhofel AL, Wilton JH, Victory JM, et al. Lack of bioequivalence of ciprofloxacin when administered with calcium-fortified orange juice: a new twist on an old interaction. J Clin Pharmacol 2002;42(4):461-6
  • Engel K, Wang J. Interaction of organic cations with a newly identified plasma membrane monoamine transporter. Mol Pharmacol 2005;68(5):1397-407
  • Pastor-Anglada M, Cano-Soldado P, Molina-Arcas M, et al. Cell entry and export of nucleoside analogues. Virus Res 2005;107(2):151-64
  • Engel K, Zhou M, Wang J. Identification and characterization of a novel monoamine transporter in the human brain. J Biol Chem 2004;279(48):50042-9
  • Koepsell H. The SLC22 family with transporters of organic cations, anions and zwitterions. Mol Aspects Med 2013;34(2-3):413-35
  • Young JD, Yao SY, Baldwin JM, et al. The human concentrative and equilibrative nucleoside transporter families, SLC28 and SLC29. Mol Aspects Med 2013;34(2-3):529-47
  • Halestrap AP, Meredith D. The SLC16 gene family-from monocarboxylate transporters (MCTs) to aromatic amino acid transporters and beyond. Pflügers Arch 2004;447(5):619-28
  • Halestrap AP. The monocarboxylate transporter family--Structure and functional characterization. IUBMB Life 2012;64(1):1-9
  • Lam WK, Felmlee MA, Morris ME. Monocarboxylate transporter-mediated transport of gamma-hydroxybutyric acid in human intestinal Caco-2 cells. Drug Metab Dispos 2010;38(3):441-7
  • Halestrap AP. The SLC16 gene family - structure, role and regulation in health and disease. Mol Aspects Med 2013;34(2-3):337-49
  • Morris ME, Felmlee MA. Overview of the proton-coupled MCT (SLC16A) family of transporters: characterization, function and role in the transport of the drug of abuse gamma-hydroxybutyric acid. AAPS J 2008;10(2):311-21
  • Li YH, Ito K, Tsuda Y, et al. Mechanism of intestinal absorption of an orally active beta-lactam prodrug: uptake and transport of carindacillin in Caco-2 cells. J Pharmacol Exp Ther 1999;290(3):958-64
  • Emoto A, Ushigome F, Koyabu N, et al. H(+)-linked transport of salicylic acid, an NSAID, in the human trophoblast cell line BeWo. Am J Physiol Cell Physiol 2002;282(5):C1064-75
  • Utoguchi N, Audus KL. Carrier-mediated transport of valproic acid in BeWo cells, a human trophoblast cell line. Int J Pharm 2000;195(1-2):115-24
  • Wu X, Whitfield LR, Stewart BH. Atorvastatin transport in the Caco-2 cell model: contributions of P-glycoprotein and the proton-monocarboxylic acid co-transporter. Pharm Res 2000;17(2):209-15
  • Okamura A, Emoto A, Koyabu N, et al. Transport and uptake of nateglinide in Caco-2 cells and its inhibitory effect on human monocarboxylate transporter MCT1. Br J Pharmacol 2002;137(3):391-9
  • Kim DK, Kanai Y, Chairoungdua A, et al. Expression cloning of a Na+-independent aromatic amino acid transporter with structural similarity to H+/monocarboxylate transporters. J Biol Chem 2001;276(20):17221-8
  • Enerson BE, Drewes LR. Molecular features, regulation, and function of monocarboxylate transporters: implications for drug delivery. J Pharm Sci 2003;92(8):1531-44
  • Gill RK, Saksena S, Alrefai WA, et al. Expression and membrane localization of MCT isoforms along the length of the human intestine. Am J Physiol Cell Physiol 2005;289(4):C846-52
  • Price NT, Jackson VN, Halestrap AP. Cloning and sequencing of four new mammalian monocarboxylate transporter (MCT) homologues confirms the existence of a transporter family with an ancient past. Biochem J 1998;329(Pt 2):321-8
  • Yoon H, Fanelli A, Grollman EF, Philp NJ. Identification of a unique monocarboxylate transporter (MCT3) in retinal pigment epithelium. Biochem Biophys Res Commun 1997;234(1):90-4
  • Philp NJ, Yoon H, Grollman EF. Monocarboxylate transporter MCT1 is located in the apical membrane and MCT3 in the basal membrane of rat RPE. Am J Physiol 1998;274(6 Pt 2):R1824-8
  • Saier MH Jr, Tran CV, Barabote RD. TCDB: the transporter classification database for membrane transport protein analyses and information. Nucleic Acids Res 2006;34(Database issue):D181-6
  • Wong K, Ma J, Rothnie A, et al. Towards understanding promiscuity in multidrug efflux pumps. Trends Biochem Sci 2014;39(1):8-16
  • Vasiliou V, Vasiliou K, Nebert DW. Human ATP-binding cassette (ABC) transporter family. Hum Genomics 2009;3(3):281-90
  • Dean M, Hamon Y, Chimini G. The human ATP-binding cassette (ABC) transporter superfamily. J Lipid Res 2001;42(7):1007-17
  • Tarling EJ, de Aguiar Vallim TQ, Edwards PA. Role of ABC transporters in lipid transport and human disease. Trends Endocrinol Metab 2013;24(7):342-50
  • Glavinas H, Krajcsi P, Cserepes J, Sarkadi B. The role of ABC transporters in drug resistance, metabolism and toxicity. Curr Drug Deliv 2004;1(1):27-42
  • Sharom FJ. ABC multidrug transporters: structure, function and role in chemoresistance. Pharmacogenomics 2008;9(1):105-27
  • Sukowati CH, Rosso N, Pascut D, et al. Gene and functional up-regulation of the BCRP/ABCG2 transporter in hepatocellular carcinoma. BMC Gastroenterol 2012;12:160
  • Juliano RL, Ling V. A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. Biochim Biophys Acta 1976;455(1):152-62
  • Ward AB, Szewczyk P, Grimard V, et al. Structures of P-glycoprotein reveal its conformational flexibility and an epitope on the nucleotide-binding domain. Proc Natl Acad Sci USA 2013;110(33):13386-91
  • Krishna R, Yu L. editors. Biopharmaceutics application in drug development. Springer, NY, USA; 2008
  • Kato M, Chiba K, Hisaka A, et al. The intestinal first-pass metabolism of substrates of CYP3A4 and P-glycoprotein-quantitative analysis based on information from the literature. Drug Metab Pharmacokinet 2003;18(6):365-72
  • Marchetti S, Mazzanti R, Beijnen JH, Schellens JH. Concise review: clinical relevance of drug drug and herb drug interactions mediated by the ABC transporter ABCB1 (MDR1, P-glycoprotein). Oncologist 2007;12(8):927-41
  • Washington N, Washington C, Wilson C. Physiological pharmaceutics: barriers to drug absorption. 2nd edition. Taylor and Francis, Inc., NY, USA; 2001
  • Pollock NL, McDevitt CA, Collins R, et al. Improving the stability and function of purified ABCB1 and ABCA4: the influence of membrane lipids. Biochim Biophys Acta 2014;1838(1):134-47
  • Loo TW, Bartlett MC, Clarke DM. Human P-glycoprotein is active when the two halves are clamped together in the closed conformation. Biochem Biophys Res Commun 2010;395(3):436-40
  • Ho GT, Moodie FM, Satsangi J. Multidrug resistance 1 gene (P-glycoprotein 170): an important determinant in gastrointestinal disease? Gut 2003;52(5):759-66
  • MacLean C, Moenning U, Reichel A, Fricker G. Closing the gaps: a full scan of the intestinal expression of P-glycoprotein, breast cancer resistance protein, and multidrug resistance-associated protein 2 in male and female rats. Drug metab Dispos 2008;36(7):1249-54
  • MacLean C, Moenning U, Reichel A, Fricker G. Regional absorption of fexofenadine in rat intestine. Eur J Pharm Sci 2010;41(5):670-4
  • Amin ML. P-glycoprotein Inhibition for Optimal Drug Delivery. Drug Target Insights 2013;7:27-34
  • Varma MV, Ashokraj Y, Dey CS, Panchagnula R. P-glycoprotein inhibitors and their screening: a perspective from bioavailability enhancement. Pharmacol Res 2003;48(4):347-59
  • Maki N, Hafkemeyer P, Dey S. Allosteric modulation of human P-glycoprotein. Inhibition of transport by preventing substrate translocation and dissociation. J Biol Chem 2003;278(20):18132-9
  • Modok S, Heyward C, Callaghan R. P-glycoprotein retains function when reconstituted into a sphingolipid- and cholesterol-rich environment. J Lipid Res 2004;45(10):1910-18
  • Constantinides PP, Wasan KM. Lipid formulation strategies for enhancing intestinal transport and absorption of P-glycoprotein (P-gp) substrate drugs: in vitro/in vivo case studies. J Pharm Sci 2007;96(2):235-48
  • Li H, Yan Z, Ning W, et al. Using rhodamine 123 accumulation in CD8 cells as a surrogate indicator to study the P-glycoprotein modulating effect of cepharanthine hydrochloride in vivo. J Biomed Biotechnol 2011;2011:281651
  • Palmeira A, Sousa E, Vasconcelos MH, Pinto MM. Three decades of P-gp inhibitors: skimming through several generations and scaffolds. Curr Med Chem 2012;19(13):1946-2025
  • Woo JS, Lee CH, Shim CK, Hwang SJ. Enhanced oral bioavailability of paclitaxel by coadministration of the P-glycoprotein inhibitor KR30031. Pharm Res 2003;20(1):24-30
  • Novak A, Carpini GD, Ruiz ML, et al. Acetaminophen inhibits intestinal P-glycoprotein transport activity. J Pharm Sci 2013;102(10):3830-7
  • Neerati P, Ganji D, Bedada SK. Study on in situ and in vivo absorption kinetics of phenytoin by modulating P-glycoprotein with verapamil in rats. Eur J Pharm Sci 2011;44(1-2):27-31
  • Zakeri-Milani P, Valizadeh H, Islambulchilar Z, et al. Investigation of the intestinal permeability of ciclosporin using the in situ technique in rats and the relevance of P-glycoprotein. Arzneimittelforschung 2008;58(4):188-92
  • Zakeri-Milani P, Damani S, Islambulchilar Z, et al. Effect of Erythromycine on the intestinal transport of cyclosporine. JBUMS 2009;11(2):7-15
  • Zakeri-Milani P, Valizadeh H, Islambulchilar Z, et al. Effect of erythromycin and clarithromycin on the intestinal transport of digoxin. Pharm Sci 2009;15(1):75-82
  • Valizadeh H, Mehtari M, Zakeri-Milani P. Evidence for enhanced intestinal absorption of digoxin by P-glycoprotein inhibitors. Trop J Pharm Res 2012;11(6):939-45
  • Jiang L, Long X, Meng Q. Rhamnolipids enhance epithelial permeability in Caco-2 monolayers. Int J Pharm 2013;446(1-2):130-5
  • Oga EF, Sekine S, Shitara Y, Horie T. P-glycoprotein mediated efflux in Caco-2 cell monolayers: the influence of herbals on digoxin transport. J Ethnopharmacol 2012;144(3):612-17
  • Bailey DG, Spence JD, Edgar B, et al. Ethanol enhances the hemodynamic effects of felodipine. Clin Invest Med 1989;12(6):357-62
  • Dahan A, Amidon GL. Grapefruit juice and its constituents augment colchicine intestinal absorption: potential hazardous interaction and the role of p-glycoprotein. Pharm Res 2009;26(4):883-92
  • Spahn-Langguth H, Langguth P. Grapefruit juice enhances intestinal absorption of the P-glycoprotein substrate talinolol. Eur J Pharm Sci 2001;12(4):361-7
  • Hanley MJ, Cancalon P, Widmer WW, Greenblatt DJ. The effect of grapefruit juice on drug disposition. Exp Opin Drug Metab Toxicol 2011;7(3):267-86
  • Ohnishi A, Matsuo H, Yamada S, et al. Effect of furanocoumarin derivatives in grapefruit juice on the uptake of vinblastine by Caco-2 cells and on the activity of cytochrome P450 3A4. Br J Pharmacol 2000;130(6):1369-77
  • Lown KS, Mayo RR, Leichtman AB, et al. Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Clin Pharmacol Ther 1997;62(3):248-60
  • Becquemont L, Verstuyft C, Kerb R, et al. Effect of grapefruit juice on digoxin pharmacokinetics in humans. Clin Pharmacol Ther 2001;70(4):311-16
  • Parker RB, Yates CR, Soberman JE, Laizure SC. Effects of grapefruit juice on intestinal P-glycoprotein: evaluation using digoxin in humans. Pharmacotherapy 2003;23(8):979-87
  • Yasui N, Kondo T, Furukori H, et al. Effects of repeated ingestion of grapefruit juice on the single and multiple oral-dose pharmacokinetics and pharmacodynamics of alprazolam. Psychopharmacology (Berl) 2000;150(2):185-90
  • Shi J, Montay G, Leroy B, Bhargava VO. Effects of itraconazole or grapefruit juice on the pharmacokinetics of telithromycin. Pharmacotherapy 2005;25(1):42-51
  • Lassoued MA, Sfar S, Bouraoui A, Khemiss F. Absorption enhancement studies of clopidogrel hydrogen sulphate in rat everted gut sacs. J Pharm Pharmacol 2012;64(4):541-52
  • Lim GE, Li T, Buttar HS. Interactions of grapefruit juice and cardiovascular medications: a potential risk of toxicity. Exp Clin Cardiol 2003;8(2):99-107
  • Konishi T, Satsu H, Hatsugai Y, et al. Inhibitory effect of a bitter melon extract on the P-glycoprotein activity in intestinal Caco-2 cells. Br J Pharmacol 2004;143(3):379-87
  • Konishi T, Satsu H, Hatsugai Y, et al. A bitter melon extract inhibits the P-glycoprotein activity in intestinal Caco-2 cells: monoglyceride as an active compound. Biofactors 2004;22(1-4):71-4
  • Engdal S, Nilsen OG. Inhibition of P-glycoprotein in Caco-2 cells: effects of herbal remedies frequently used by cancer patients. Xenobiotica 2008;38(6):559-73
  • Hennessy M, Kelleher D, Spiers JP, et al. St Johns wort increases expression of P-glycoprotein: implications for drug interactions. Br J Clin Pharmacol 2002;53(1):75-82
  • Zhou S, Chan E, Pan SQ, et al. Pharmacokinetic interactions of drugs with St John's wort. J Psychopharmacol 2004;18(2):262-76
  • Fortuna A, Alves G, Falcao A, Soares-da-Silva P. Evaluation of the permeability and P-glycoprotein efflux of carbamazepine and several derivatives across mouse small intestine by the Ussing chamber technique. Epilepsia 2012;53(3):529-38
  • Zhang C, Zuo Z, Kwan P, Baum L. In vitro transport profile of carbamazepine, oxcarbazepine, eslicarbazepine acetate, and their active metabolites by human P-glycoprotein. Epilepsia 2011;52(10):1894-904
  • Karlsson L, Green H, Zackrisson AL, et al. ABCB1 gene polymorphisms are associated with fatal intoxications involving venlafaxine but not citalopram. Int J Legal Med 2013;127(3):579-86
  • Lin JH, Yamazaki M. Role of P-glycoprotein in pharmacokinetics: clinical implications. Clin Pharmacokinet 2003;42(1):59-98
  • Wetterich U, Spahn-Langguth H, Mutschler E, et al. Evidence for intestinal secretion as an additional clearance pathway of talinolol enantiomers: concentration- and dose-dependent absorption in vitro and in vivo. Pharm Res 1996;13(4):514-22
  • Stephens RH, O'Neill CA, Warhurst A, et al. Kinetic profiling of P-glycoprotein-mediated drug efflux in rat and human intestinal epithelia. J Pharm Exp Ther 2001;296(2):584-91
  • Ueda CT, Lemaire M, Gsell G, et al. Apparent dose-dependent oral absorption of cyclosporin A in rats. Biopharm Drug Dispos 1984;5(2):141-51
  • Guo Y, Luo J, Tan S, et al. The applications of Vitamin E TPGS in drug delivery. Eur J Pharm Sci 2013;49(2):175-86
  • Wempe MF, Wright C, Little JL, et al. Inhibiting efflux with novel non-ionic surfactants: rational design based on vitamin E TPGS. Int J Pharm 2009;370(1-2):93-102
  • Collnot EM, Baldes C, Schaefer UF, et al. Vitamin E TPGS P-glycoprotein inhibition mechanism: influence on conformational flexibility, intracellular ATP levels, and role of time and site of access. Mol Pharm 2010;7(3):642-51
  • Constantinides PP, Han J, Davis SS. Advances in the use of tocols as drug delivery vehicles. Pharm Res 2006;23(2):243-55
  • Parsa A, Saadati R, Abbasian Z, et al. Enhanced permeability of Etoposide across everted sacs of rat small intestine by vitamin E-TPGS. Iran J Pharm Res 2013;12(Suppl):37-46
  • Dintaman JM, Silverman JA. Inhibition of P-glycoprotein by D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS). Pharm Res 1999;16(10):1550-6
  • Hodaee D, Baradaran B, Valizadeh H, et al. The effect of Tween excipients on expression and activity of P-glycoprotein in Caco-2 cells. Pharmind 2014. [Epub ahead of print]
  • Yu H, Hu YQ, Ip FC, et al. Intestinal transport of bis(12)-hupyridone in Caco-2 cells and its improved permeability by the surfactant Brij-35. Biopharm Drug Dispos 2011;32(3):140-50
  • Lo YL. Relationships between the hydrophilic-lipophilic balance values of pharmaceutical excipients and their multidrug resistance modulating effect in Caco-2 cells and rat intestines. J Control Release 2003;90(1):37-48
  • Lo YL, Huang JD. Effects of sodium deoxycholate and sodium caprate on the transport of epirubicin in human intestinal epithelial Caco-2 cell layers and everted gut sacs of rats. Biochem Pharmacol 2000;59(6):665-72
  • Wang Y, Sun J, Zhang T, et al. Enhanced oral bioavailability of tacrolimus in rats by self-microemulsifying drug delivery systems. Drug Dev Ind Pharm 2011;37(10):1225-30
  • Wang Y, Guo M, Lu Y, et al. Alpha-tocopheryl polyethylene glycol succinate-emulsified poly(lactic-co-glycolic acid) nanoparticles for reversal of multidrug resistance in vitro. Nanotechnology 2012;23(49):495103
  • Ma L, Wei Y, Zhou Y, et al. Effects of Pluronic F68 and Labrasol on the intestinal absorption and pharmacokinetics of rifampicin in rats. Arch Pharm Res 2011;34(11):1939-43
  • Dunnhaupt S, Barthelmes J, Rahmat D, et al. S-protected thiolated chitosan for oral delivery of hydrophilic macromolecules: evaluation of permeation enhancing and efflux pump inhibitory properties. Mol Pharm 2012;9(5):1331-41
  • Simon S, Schubert R. Inhibitory effect of phospholipids on P-glycoprotein: cellular studies in Caco-2, MDCKII mdr1 and MDCKII wildtype cells and P-gp ATPase activity measurements. Biochim Biophys Acta 2012;1821(9):1211-23
  • Negi LM, Tariq M, Talegaonkar S. Nano scale self-emulsifying oil based carrier system for improved oral bioavailability of camptothecin derivative by P-Glycoprotein modulation. Colloids Surf B Biointerfaces 2013;111C:346-53
  • Shen Q, Lin Y, Handa T, et al. Modulation of intestinal P-glycoprotein function by polyethylene glycols and their derivatives by in vitro transport and in situ absorption studies. Int J Pharm 2006;313(1-2):49-56
  • Hugger ED, Audus KL, Borchardt RT. Effects of poly(ethylene glycol) on efflux transporter activity in Caco-2 cell monolayers. J Pharm Sci 2002;91(9):1980-90
  • Mohammadzadeh R, Baradaran B, Valizadeh H, et al. Reduced ABCB1 expression and activity in the presence of acrylic copolymers. Advanced Pharmaceutical Bulletin 2014;4(3):219-24

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