Assessment of blood-brain barrier permeability using the in situ mouse brain perfusion technique

Pharmaceutical Research

Volumn 26, Issue 7, 2009, Pages 1657-1664

  Zhao, Rong ^a   Kalvass, J Cory ^b   Pollack, Gary M ^a  

^a UNIVERSITY OF NORTH CAROLINA   (United States)

^b ELI LILLY AND COMPANY   (United States)

Author keywords

Blood brain barrier; Permeability; Protein binding; Time to equilibrium

Indexed keywords

ALFENTANIL; COLCHICINE; DIAZEPAM; FEXOFENADINE; GLYCOPROTEIN P; PHENYTOIN; QUINIDINE; RITONAVIR; SUFENTANIL; TERFENADINE; VALPROIC ACID; VERAPAMIL;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; BLOOD FLOW VELOCITY; BRAIN PERFUSION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG CLEARANCE; DRUG UPTAKE; LIPOPHILICITY; MEMBRANE PERMEABILITY; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING;

ANIMALS; BLOOD FLOW VELOCITY; BLOOD-BRAIN BARRIER; BRAIN; LIPIDS; MICE; MICE, KNOCKOUT; P-GLYCOPROTEINS; PERFUSION; PERMEABILITY; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS;

EID: 67349191878     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-009-9876-4     Document Type: Article

References (39)

1. RP Meyer M Gehlhaus R Knoth B Volk 2007 Expression and function of cytochrome p450 in brain drug metabolism Curr Drug Metab 8 297 306 10.2174/138920007780655478
2. DJ Begley 2003 Understanding and circumventing the blood-brain barrier Acta Paediatr Suppl 92 83 91 10.1080/08035320310020904
3. G Miller 2002 Drug targeting. Breaking down barriers. Science 297 1116 8 10.1126/science.297.5584.1116
4. AH Schinkel 1999 P-Glycoprotein, a gatekeeper in the blood-brain barrier Adv Drug Deliv Rev 36 179 94 10.1016/S0169-409X(98)00085-4
5. X Liuand C Chen 2005 Strategies to optimize brain penetration in drug discovery Curr Opin Drug Discov Devel 8 505 12
6. JD Fenstermacher RG Blasberg CS Patlak 1981 Methods for quantifying the transport of drugs across brain barrier systems Pharmacol Ther 14 217 48 10.1016/0163-7258(81)90062-0
7. JC Kalvassand TS Maurer 2002 Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery Biopharm Drug Dispos 23 327 38 10.1002/bdd.325
8. JC Kalvass TS Maurer GM Pollack 2007 Use of plasma and brain unbound fractions to assess the extent of brain distribution of 34 drugs: comparison of unbound concentration ratios to in vivo p-glycoprotein efflux ratios Drug Metab Dispos 35 660 6 10.1124/dmd.106.012294
9. JC Kalvass CL Graff GM Pollack 2004 Use of loperamide as a phenotypic probe of mdr1a status in CF-1 mice Pharm Res 21 1867 70 10.1023/B:PHAM. 0000045241.26925.8b
10. AH Schinkel JJ Smit O van Tellingen JH Beijnen E Wagenaar L van Deemter 1994 Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs Cell 77 491 502 10.1016/0092-8674(94)90212-7
11. WM Pardridge 2004 Log(BB), PS products and in silico models of drug brain penetration Drug Discov Today 9 392 3 10.1016/S1359-6446(04)03065-X
12. I Martin 2004 Prediction of blood-brain barrier penetration: are we missing the point Drug Discov Today 9 161 2 10.1016/S1359-6446(03)02961-1
13. X Liu M Tu RS Kelly C Chen BJ Smith 2004 Development of a computational approach to predict blood-brain barrier permeability Drug Metab Dispos 32 132 9 10.1124/dmd.32.1.132
14. Smith QR. Brain perfusion systems for studies of drug uptake and metabolism in the central nervous system. In: Borchardt RT, editor. Models for assessing drug absorption and metabolism. New York: Plenum; 1996.
15. Y Takasato SI Rapoport QR Smith 1984 An in situ brain perfusion technique to study cerebrovascular transport in the rat Am J Physiol 247 H484 93
16. H Murakami H Takanaga H Matsuo H Ohtani Y Sawada 2000 Comparison of blood-brain barrier permeability in mice and rats using in situ brain perfusion technique Am J Physiol Heart Circ Physiol 279 H1022 8
17. C Dagenais CL Graff GM Pollack 2004 Variable modulation of opioid brain uptake by P-glycoprotein in mice Biochem Pharmacol 67 269 76 10.1016/j.bcp.2003.08.027
18. C Dagenais C Rousselle GM Pollack JM Scherrmann 2000 Development of an in situ mouse brain perfusion model and its application to mdr1a P-glycoprotein-deficient mice J Cereb Blood Flow Metab 20 381 6 10.1097/00004647-200002000-00020
19. C Dagenais J Zong J Ducharme GM Pollack 2001 Effect of mdr1a P-glycoprotein gene disruption, gender, and substrate concentration on brain uptake of selected compounds Pharm Res 18 957 63 10.1023/A:1010984110732
20. X Liu BJ Smith C Chen E Callegari SL Becker X Chen 2005 Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: an experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding J Pharmacol Exp Ther 313 1254 62 10.1124/jpet.104.079319
21. WM Pardridge 2005 The blood-brain barrier: bottleneck in brain drug development NeuroRx 2 3 14 10.1602/neurorx.2.1.3
22. J Lotsch 2005 Pharmacokinetic-pharmacodynamic modeling of opioids J Pain Symptom Manage 29 S90 103 10.1016/j.jpainsymman.2005.01.012
23. T Obradovic GG Dobson T Shingaki T Kungu IJ Hidalgo 2007 Assessment of the first and second generation antihistamines brain penetration and role of P-glycoprotein Pharm Res 24 318 27 10.1007/s11095-006-9149-4
24. H Tahara H Kusuhara E Fuse Y Sugiyama 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 8 10.1124/dmd.105.004192
25. TS Maurer DB Debartolo DA Tess DO Scott 2005 Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice Drug Metab Dispos 33 175 81 10.1124/dmd.104.001222
26. KD Adkisonand DD Shen 1996 Uptake of valproic acid into rat brain is mediated by a medium-chain fatty acid transporter J Pharmacol Exp Ther 276 1189 200
27. C Anthonypillai RN Sanderson JE Gibbs SA Thomas 2004 The distribution of the HIV protease inhibitor, ritonavir, to the brain, cerebrospinal fluid, and choroid plexuses of the guinea pig J Pharmacol Exp Ther 308 912 20 10.1124/jpet.103.060210
28. BB Brodie H Kurz LS Schanker 1960 The importance of dissociation constant and lipid-solubility in influencing the passage of drugs into the cerebrospinal fluid J Pharmacol Exp Ther 130 20 5
29. WH Oldendorf 1974 Lipid solubility and drug penetration of the blood brain barrier Proc Soc Exp Biol Med 147 813 5
30. H van de Waterbeemd G Camenisch G Folkers JR Chretien OA Raevsky 1998 Estimation of blood-brain barrier crossing of drugs using molecular size and shape, and H-bonding descriptors J Drug Target 6 151 65
31. KM Mahar Doan SA Wring LJ Shampine KH Jordan JP Bishop J Kratz 2004 Steady-state brain concentrations of antihistamines in rats: interplay of membrane permeability, P-glycoprotein efflux and plasma protein binding Pharmacology 72 92 8 10.1159/000079137
32. R Zhao JC Kalvass S Yanni AS Bridges GM Pollack 2009 Fexofenadine brain exposure and the influence of blood-brain barrier P-glycoprotein following fexofenadine and terfenadine administration Drug Metab and Dispos 37 529 35 10.1124/dmd.107.019893
33. KM Mahar Doan JE Humphreys LO Webster SA Wring LJ Shampine CJ Serabjit-Singh 2002 Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs J Pharmacol Exp Ther 303 1029 37 10.1124/jpet.102.039255
34. JC Kalvass ER Olson MP Cassidy DE Selley GM Pollack 2007 Pharmacokinetics and Pharmacodynamics of seven opioids in P-gp-competent mice: assessment of unbound brain EC50 and correlation of in vitro, preclinical, and clinical data J Pharmacol Exp Ther 323 346 55 10.1124/jpet.107.119560
35. JC Kalvass ER Olson GM Pollack 2007 Pharmacokinetics and pharmacodynamics of alfentanil in P-glycoprotein-competent and P-glycoprotein-deficient mice: P-glycoprotein efflux alters alfentanil brain disposition and antinociception Drug Metab Dispos 35 455 9 10.1124/dmd.106.011445
36. JC Kalvassand GM Pollack 2007 Kinetic considerations for the quantitative assessment of efflux activity and inhibition: implications for understanding and predicting the effects of efflux inhibition Pharm Res 24 265 76 10.1007/s11095-006-9135-x
37. M Hammarlund-Udenaes LK Paalzow EC de Lange 1997 Drug equilibration across the blood-brain barrier-pharmacokinetic considerations based on the microdialysis method Pharm Res 14 128 34 10.1023/A:1012080106490
38. SG Summerfield K Read DJ Begley T Obradovic IJ Hidalgo S Coggon 2007 Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction J Pharmacol Exp Ther 322 205 13 10.1124/jpet.107.121525
39. R Deaneand MW Bradbury 1990 Transport of lead-203 at the blood-brain barrier during short cerebrovascular perfusion with saline in the rat J Neurochem 54 905 14 10.1111/j.1471-4159.1990.tb02337.x