Blood-brain barrier in vitro models as tools in drug discovery: Assessment of the transport ranking of antihistaminic drugs

Pharmazie

Volumn 67, Issue 5, 2012, Pages 432-439

  Neuhaus, Winfried ^a,d   Mandikova, J ^a,b   Pawlowitsch, R ^a   Linz, B ^c   Bennani Baiti, B ^a   Lauer, R ^a   Lachmann, B ^a   Noe, C R ^a  

^a UNIVERSITY OF VIENNA   (Austria)

^b Charles University in Prague Faculty of Pharmacy   (Czech Republic)

^c GOETHE UNIVERSITY   (Germany)

^d UNIVERSITY OF WÜRZBURG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIHISTAMINIC AGENT; ASTEMIZOLE; CETIRIZINE; DIAZEPAM; DIPHENHYDRAMINE; FEXOFENADINE; GLYCOPROTEIN P; LORATADINE; PHENIRAMINE; PROMETHAZINE; RHODAMINE 123; VERAPAMIL;

ANIMAL CELL; ARTICLE; BLOOD BRAIN BARRIER; CENTRAL NERVOUS SYSTEM; DRUG DEVELOPMENT; DRUG PENETRATION; DRUG TRANSPORT; ENDOTHELIUM CELL; HUMAN; HUMAN CELL; MOUSE; NONHUMAN; RAT; TRANSCYTOSIS;

ALGORITHMS; ANIMALS; BIOLOGICAL TRANSPORT, ACTIVE; BLOOD-BRAIN BARRIER; CELL LINE; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DRUG DISCOVERY; FLUORESCENT DYES; HISTAMINE ANTAGONISTS; MICROSCOPY, FLUORESCENCE; MODELS, BIOLOGICAL; P-GLYCOPROTEIN; PERMEABILITY; RATS; RHODAMINE 123;

EID: 84862322700     PISSN: 00317144     EISSN: None     Source Type: Journal    
DOI: 10.1691/ph.2012.1742     Document Type: Article

References (63)

1. Abbott NJ, Rönnbäck L, Hansson E (2006) Astrocyte-endothelial interactions at the blood-brain barrier. Nat Rev Neurosci 7: 41-53.
2. André P, Debray M, Scherrmann JM, Cisternino S (2009) Clonidine transport at the mouse blood-brain barrier by a new H+ antiporter that interacts with addictive drugs. J Cereb Blood Flow Metab 29: 1293-1304.
3. Bauer B, Hartz AM, Fricker G, Miller DS (2005) Modulation of p-glycoprotein transport function at the blood-brain barrier. Exp Biol Med 230: 118-127.
4. Benda P, Lightbody J, Sato G, Levine L, Sweet W (1968) Differential rat glial cell strain in tissue culture. Science 161: 370-371.
5. Bennani B, Noe CR (2009) Drug transporters in health and disease, in: Ecker G, Chiba P (Eds.) Transporters as Drug Carriers: Structure, Function, Substrates: 44 (Methods and Principles in Medicinal Chemistry), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, Germany, pp. 383-413.
6. Bjerrum OJ (2000) New safe medicines faster: A proposal for a key action within the European union's 6th framework programme. Pharmacol Toxicol 86: 23-26.
7. Camelo-Nunes IC (2006) New antihistamines: a critical view. J Pediatr 82: 173-180.
8. Cattelotte J, Tournier N, Rizzo-Padoin N, Schinkel AH, Scherrmann JM, Cisternino S (2009) Changes in dipole membrane potential at the mouse blood-brain barrier enhance the transport of 99mTechnetium Sestamibi more than inhibiting Abcb1, Abcc1, or Abcg2. J Neurochem 108: 767-775.
9. Chen C, Hanson E, Watson JW, Lee JS (2003) P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonists. Drug Metab Dispos 31: 312-318.
10. Dagenais C, Ducharme J, Pollack GM (2001) Uptake and efflux of the peptidic delta-opioid receptor agonist. Neurosci Lett 301: 155-158.
11. Depoortere H, Decobert M, Granger P, Françon D (1995) Mizolastine, a novel selective histamine H1 receptor antagonist: lack of sedative potential on the EEG in the rodent. Neuropsychobiology 32: 214-221.
12. Dönmez Y, Akhmetova L, Işeri OD, Kars MD, Gündüz U (2011) Effect of MDR modulators verapamil and promethazine on gene expression levels of MDR1 and MRP1 in doxorubicin-resistant MCF-7 cells. Cancer Chemother Pharmacol 67: 823-828.
13. Ecker GF, Noe CR (2006) In silico prediction models for blood-brain barrier permeation, in: Dermietzel R, Spray DC, Nedergaard M, (eds.) Bloodbrain barriers: from ontogeny to artificial interfaces, Volume 1. Wiley-VCH Verlag GmbH & Co.KGaA, Weinheim, Germany, pp.403-428.
14. Fischer W, Neubert RHH, Brandsch M (2007) Clonidine accumulation in human neuronal cells. Eur J Pharm Sci 32: 291-295.
15. Goldberg MJ, Spector R, Chiang CK (1987) Transport of diphenhydramine in the central nervous system. J Pharmacol Exp Ther 240: 717-722.
16. Gonzales MA, Estes KS (1998) Pharmacokinetic overview of oral secondgeneration H1 antihistamines. Int J Clin Pharmaco Ther 36: 292-300.
17. Hakala KS, Laitinen L, Kaukonen AM, Hirvonen J, Kostiainen R, Kotiaho T (2003) Development of LC/MS/MS methods for cocktail dosed Caco-2 samples using atmospheric pressure photoionization and electrospray ionization. Anal Chem 75: 5969-5977.
18. Han YH, Sweet DH, Hu dN, Pritchard JB (2001) Characterization of a novel cationic drug transporter in human retinal pigment epithelial cells. J Pharmacol Exp Ther 296: 450-457.
19. Handley DA, Magnetti A, Higgens AJ (1998) Therapeutic advantages of third generation antihistamines. Expert Opin Investig Drugs 7: 1045-1054.
20. He Y, Liu Y, Zeng S (2010) Stereoselective and multiple carrier-mediated transport of cetirizine across Caco-2 cell monolayers with potential drug interaction. Chirality 22: 684-692.
21. Hoffmann K, Grafe F, Wohlrab W, Neubert RH, Brandsch M (2002) Functional characterization of a high-affinity choline transport system in human keratinocytes. J Invest Dermatol 119: 118-121.
22. Jonkman JH,Westenberg HG, Rijntjes NV, van der Kleijn E, Lindeboom SF (1983) Whole body distribution of the quaternary ammonium compound thiazinamium (N-methylpromethazine) and promethazine in monkey and mice. Arzneimittelforschung 33: 223-228.
23. Kalliokoski A, Niemi M (2009) Impact of OATP transporters on pharmacokinetics. Br J Pharmacol 158: 693-705.
24. Kars MD, Işeri OD, Gunduz U, Molnar J (2008) Reversal of multidrug resistance by synthetic and natural compounds in drug-resistant MCF-7 cell lines. Chemotherapy 54: 194-200.
25. Kay GG (2000) The effects of antihistamines on cognition and performance. J Allergy Clin immunol 105: S622-S627.
26. Kay GG, Harris AG (1999) Loratadine: a non-sedating antihistamine. Review of its effects on cognition, psychomotor performance, mood and sedation. Clin Exp Allergy 29: 147-150.
27. Koljonen M, Hakala KS, Ahtola-Satila T, Laitinen L, Kostiainen R, Kotiaho T, Kaukonen AM, Hirvonen J (2006) Evaluation of cocktail approach to standardise Caco-2 permeability experiments. Eur J Pharm Biopharm 64: 379-387.
28. Lappin G, Shishikura Y, Jochemsen R, Weaver RJ, Gesson C, Housten B, Oosterhuis B, Bjerrum OJ, Rowland M, Garner C (2010) Pharmacokinetics of fexofenadine: evaluation of a microdose and assessment of absolute oral bioavailability. Eur J Pharm Sci 40: 125-131.
29. Lauer R, Bauer R, Linz B, Pittner F, Peschek GA, Ecker G, Friedl P, Noe CR (2004) Development of an in vitro blood-brain barrier model based on immortalized porcine brain microvascular endothelial cells. Farmaco 59: 133-137.
30. Mahringer A, Karamustafa S, Klotz D, Kahl S, Konkimalla VB, Wang Y, Wang J, Liu HY, Boechzelt H, Hao X, Bauer R, Fricker G, Efferth T (2010) Inhibition of P-glycoprotein at the blood-brain barrier by phytochemicals derived from traditional Chinese medicine. Cancer Genomics Proteomics 7: 191-205.
31. Marzanatti M, Monopoli A, Trampus M, Ongini E (1989) Effects of nonsedating histamine H1-antagonists on EEG activity and behavior in the cat. Pharmacol Biochem Behav 32: 861-866.
32. Mealey KL, Waiting D, Raunig DL, Schmidt KR, Nelson FR (2010) Oral bioavailability of P-glycoprotein substrate drugs do not differ between ABCB1-1Δ and ABCB1 wild type dogs. J Vet Pharmacol Ther 33: 453-460.
33. Meeves SG, Appajosyla S (2003) Efficacy and safety profile of fexofenadine HCl: a unique therapeutic option in H1-receptor antagonist treatment. J Allergy Clin Immunol 112: S69-S77.
34. Meltzer EO (1990) Antihistamine- and decongestant-induced performance decrements. J Occup Med 32: 327-334.
35. Meyer J, Rauh J, Galla HJ (1991) The susceptibility of cerebral endothelial cells to astroglial induction of blood-brain barrier enzymes depends on their proliferative state. J Neurochem 57: 1971-1977.
36. Molimard M, Diquet B, Benedetti MS (2004) Comparison of pharmacokinetics and metabolism of desloratadine, fexofenadine, levocetirizine and mizolastine in humans. Fundam Clin Pharmacol 18: 399-411.
37. Neuhaus W, Bogner E, Wirth M, Trzeciak J, Lachmann B, Gabor F, Noe CR (2006a) A Novel Tool to Characterize Paracellular Transport: The APTS-Dextran Ladder. Pharm Res 23: 1491-1501.
38. Neuhaus W, Lauer R, Oelzant S, Fringeli UP, Ecker GF, Noe CR (2006b) A novel flow based hollow-fiber blood-brain barrier in vitro model with immortalised cell line PBMEC/C1-2. J Biotechnol 125: 127-141.
39. Neuhaus W, Trauner G, Gruber D, Oelzant S, Klepal W, Kopp B, Noe CR (2008a) Transport of a GABAA receptor modulator and its derivatives from Valeriana officinalis L. s. l. across an in vitro cell culture model of the blood-brain barrier. Planta Med 74: 1338-1344.
40. Neuhaus W, Plattner VE, Wirth M, Germann B, Lachmann B, Gabor F, Noe CR (2008b) Validation of in vitro cell culture models of the blood-brain barrier: Tightness characterization of two promising cell lines. J Pharm Sci 97: 5158-5175.
41. Neuhaus W, Stessl M, Strizsik E, Bennani-Baiti B, Wirth M, Toegel S, Modha M, Winkler J, Gabor F, Viernstein H, Noe CR (2010) Blood-brain barrier cell line PBMEC/C1-2 possesses functionally active P-glycoprotein. Neurosci Lett 469: 224-228.
42. Obradovic T, Dobson GG, Shingaki T, Kungu T, Hidalgo IJ (2007) Assessment of the first and second generation antihistamines brain penetration and role of P-glycoprotein. Pharm Res 24: 318-327.
43. Pottiez G, Deracinois B, Duban-Deweer S, Cecchelli R, Fenart L, Karamanos Y, Flahaut C (2010) A large-scale electrophoresis- and chromatography-based determination of gene expression profiles in bovine brain capillary endothelial cells after the re-induction of bloodbrain barrier properties. Proteome Sci 8: 57.
44. Ridout F, Hindmarch I (2003). The effects of acute doses of fexofenadine, promethazine, and placebo on cognitive and psychomotor function in healthy Japanese volunteers. Ann Allergy Asthma Immunol 90: 404-410.
45. Roux F, Couraud PO (2005) Rat brain endothelial cell lines for the study of blood-brain barrier permeability and transport functions. Cell Mol Neurobiol 25: 41-58.
46. Schinkel AH (1999) P-Glycoprotein, a gatekeeper in the blood-brain barrier. Adv Drug Deliv Rev 36: 179-194.
47. Sheu MT, Liou YB, Kao YH, Lin YK, Ho HO (2010) A quantitative structure-activity relationship fort he modulation effects of flavonoids on p-glycoprotein-mediated transport. Chem Pharm Bull (Tokyo) 58: 1187-1194.
48. Silwedel C, Förster C (2006) Differential susceptibility of cerebral and cerebellar murine brain microvascular endothelial cells to loss of barrier properties in response to inflammatory stimuli. J Neuroimmunol 179: 37-45.
49. Simons FER (1994) H1-receptor antagonists. Comparative tolerability and safety. Drug Saf 10: 350-380.
50. Smalley J, Kadiyala P, Xin B, Balimane P, Olah T (2006) Development of an on-line extraction turbulent flow chromatography tandem mass spectrometry method for cassette analysis of Caco-2 cell based bi-directional assay samples. J Chromatography B 830: 270-277.
51. Stanness KA, Neumaier JF, Sexton TJ, Grant GA, Emmi A, Maris DO, Janigro D (1999) A new model of the blood-brain barrier: co-culture of neuronal, endothelial and glial cells under dynamic conditions. Neuroreport 10: 3725-3731.
52. Suda K, Rothen-Rutishauser B, Gunthert M, Wunderli-Allenspach H (2001) Phenotypic characterization of human umbivilical vein endothelial (ECV304) and urinary carcinoma (T24) cells: endothelial vs. epithelial features. In vitro Cell Dev Biol Anim 37: 505-514.
53. Tahara H, Kusuhara H, Fuse E, Sugiyama Y (2005) P-glycoprotein plays a major role in the efflux of fexofenadine in the small intestine and blood-brain barrier, but only a limited role in its biliary excretion. Drug Metab Dispos 33: 963-968.
54. Thanabalasundaram G, Schneidewind J, Pieper C, Galla HJ (2011) The impact of pericytes on the blood-brain barrier integrity depends critically on the pericyte differentiation stage. Int J Biochem Cell Biol 43: 1284-1293.
55. Tian X, Zamek-Gliszczynski MJ, Li J, Bridges AS, Nezasa K, Patel NJ, Raub TJ, Brouwer KL (2008) Multidrug resistance-associated protein 2 is primarily responsible for the biliary excretion of fexofenadine in mice. Drug Metab Dispos 36: 61-64.
56. Teifel M, Friedl P (1996) Establishment of the permanent microvascular endothelial cell line PBMEC/C1-2 from porcine brains. Exp Cell Res 228:50-57.
57. Weksler BB, Subileau EA, Perrière N, Charneau P, Holloway K, Leveque M, Tricoire-Leignel H, Nicotra A, Bourdoulous S, Turowski P, Male DK, Roux F, Greenwood J, Romero IA, Couraud PO (2005) Blood-brain barrier-specific properties of a human adult brain endothelial cell line. FASEB J 19: 1872-1884.
58. Williams D (2004) The critical path to medical innovation. Med Device Technol 15: 8-10.
59. Yamazaki M, Fukuoka H, Nagata O, Kato H, Ito Y, Terasaki T, Tsuji A (1994) Transport mechanism of an H1-antagonist at the blood-brain barrier: transport mechanism of mepyramine using the carotid injection technique. Biol Pharm Bull 17: 676-9.
60. Yang ZH, Liu XD (2008) P-glycoprotein-mediated efflux of phenobarbital at the blood-brain barrier evidence from transport experiments in vitro. Epilepsy Res 78: 40-49.
61. Zhao R, Pollack GM (2009) Regional differences in capillary density, perfusion rate, and P-glycoprotein activity: a quantitative analysis of regional drug exposure in the brain. Biochem Pharmacol 78: 1052-1059.
62. Zhao R, Kalvass JC, Pollack GM (2009a) Assessment of blood-brain barrier permeability using the in situ mouse brain perfusion technique. Pharm Res 26: 1657-1664.
63. Zhao R, Kalvass JC, Yanni SB, Bridges AS, Pollack GM (2009b) Fexofenadine brain exposure and the influence of blood-brain barrier P-glycoprotein after fexofenadine and terfenadine administration. Drug Metab Dispos 37: 529-535.