Case study: Adapting in vitro blood-brain barrier models for use in early-stage drug discovery

Drug Discovery Today

Volumn 17, Issue 7-8, 2012, Pages 285-290

  Vandenhaute, Elodie ^a,b,c   Sevin, Emmanuel ^a,b,c   Hallier Vanuxeem, Dorothée ^a,b,c   Dehouck, Marie Pierre ^a,b,c   Cecchelli, Roméo ^a,b,c  

^a UNIV LILLE   (France)

^b UArtois   (France)

^c IMPRT IFR114   (France)

Author keywords

[No Author keywords available]

Indexed keywords

BLOOD BRAIN BARRIER; CELL MEMBRANE PERMEABILITY; DRUG INDUSTRY; DRUG RESEARCH; IN VITRO STUDY; REVIEW;

EID: 84859266457     PISSN: 13596446     EISSN: 18785832     Source Type: Journal    
DOI: 10.1016/j.drudis.2011.10.006     Document Type: Short Survey

References (30)

1. P. Jeffrey, and S. Summerfield Assessment of the blood-brain barrier in CNS drug discovery Neurobiol. Dis. 37 2010 33 37
2. L. Di Strategies to assess bloodbrain barrier penetration Expert Opin. Drug Discov. 3 2008 677 687 (Pubitemid 351890679)
3. T.A. Aasmundstad Distribution of morphine 6-glucuronide and morphine across the blood-brain barrier in awake, freely moving rats investigated by in vivo microdialysis sampling J. Pharmacol. Exp. Ther. 275 1995 435 441
4. D.A. Smith The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery Nat. Rev. Drug Discov. 9 2010 929 939
5. M. Hammarlund-Udenaes On the rate and extent of drug delivery to the brain Pharm. Res. 25 2008 1737 1750
6. Y. Takasato An in situ brain perfusion technique to study cerebrovascular transport in the rat Am. J. Physiol. 247 1984 484 493
7. A. Reichel The role of blood-brain barrier studies in the pharmaceutical industry Curr. Drug Metab. 7 2006 183 203
8. A. Toth Patented in vitro blood-brain barrier models in CNS drug discovery Recent Pat. CNS Drug Discov. 6 2011 107 118
9. M. Gumbleton, and K.L. Audus Progress and limitations in the use of in vitro cell cultures to serve as a permeability screen for the blood-brain barrier J. Pharm. Sci. 90 2001 1681 1698 (Pubitemid 33062590)
10. O. Lacombe In vitro primary human and animal cell-based blood-brain barrier models as a screening tool in drug discovery Mol. Pharm. 8 2011 651 663
11. L. Di Comparison of blood-brain barrier permeability assays: in situ brain perfusion, MDR1-MDCKII and PAMPA-BBB J. Pharm. Sci. 98 2009 1980 1991
12. I. Pastan A retrovirus carrying an MDR1 cDNA confers multidrug resistance and polarized expression of P-glycoprotein in MDCK cells Proc. Natl. Acad. Sci. U.S.A. 85 1988 4486 4490
13. Y. Xiao A 96-well efflux assay to identify ABCG2 substrates using a stably transfected MDCK II cell line Mol. Pharm. 3 2006 45 54 (Pubitemid 43331750)
14. P.A. Nielsen Models for predicting blood-brain barrier permeation Drug Discov. Today 16 2011 472 475
15. S.G. Summerfield Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction J. Pharmacol. Exp. Ther. 322 2007 205 213 (Pubitemid 46956363)
16. M.P. Dehouck An easier, reproducible, and mass-production method to study the blood-brain barrier in vitro J. Neurochem. 54 1990 1798 1801
17. Y. Zhang Porcine brain microvessel endothelial cells as an in vitro model to predict in vivo blood-brain barrier permeability Drug Metab. Dispos. 34 2006 1935 1943 (Pubitemid 44771724)
18. S. Nakagawa A new blood-brain barrier model using primary rat brain endothelial cells, pericytes and astrocytes Neurochem. Int. 54 2009 253 263
19. C. Coisne Mouse syngenic in vitro blood-brain barrier model: a new tool to examine inflammatory events in cerebral endothelium Lab. Invest. 85 2005 734 746 (Pubitemid 40799703)
20. V. Josserand Evaluation of drug penetration into the brain: a double study by in vivo imaging with positron emission tomography and using an in vitro model of the human blood-brain barrier J. Pharmacol. Exp. Ther. 316 2006 79 86 (Pubitemid 41832583)
21. S. Hamm Astrocyte mediated modulation of blood-brain barrier permeability does not correlate with a loss of tight junction proteins from the cellular contacts Cell Tissue Res. 315 2004 157 166 (Pubitemid 38657422)
22. C. Mysiorek Peroxisome-proliferator-activated receptor-alpha activation protects brain capillary endothelial cells from oxygen-glucose deprivation-induced hyperpermeability in the blood-brain barrier Curr. Neurovasc. Res. 6 2009 181 193
23. S. Lundquist Prediction of drug transport through the blood-brain barrier in vivo: a comparison between two in vitro cell models Pharm. Res. 19 2002 976 981 (Pubitemid 34804239)
24. M. Culot An in vitro blood-brain barrier model for high throughput (HTS) toxicological screening Toxicol. In Vitro 22 2008 799 811
25. V. Berezowski Contribution of glial cells and pericytes to the mRNA profiles of P-glycoprotein and multidrug resistance-associated proteins in an in vitro model of the blood-brain barrier Brain Res. 1018 2004 1 9 (Pubitemid 38942854)
26. H. Wan High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery J. Med. Chem. 50 2007 4606 4615 (Pubitemid 47463235)
27. Y.J. Yu Boosting brain uptake of a therapeutic antibody by reducing its affinity for a transcytosis target Sci. Transl. Med. 3 2011 84ra44
28. S. Levenberg Isolation, differentiation and characterization of vascular cells derived from human embryonic stem cells Nat. Protoc. 5 2010 1115 1126
29. D. James Expansion and maintenance of human embryonic stem cell-derived endothelial cells by TGFβ inhibition is Id1 dependent Nat. Biotechnol. 28 2010 161 166
30. Y. Asai Combination of functional cardiomyocytes derived from human stem cells and a highly-efficient microelectrode array system: an ideal hybrid model assay for drug development Curr. Stem Cell Res. Ther. 5 2010 227 232