In vitro blood-brain barrier permeability of nevirapine compared to other HIV antiretroviral agents

Journal of Pharmaceutical Sciences

Volumn 87, Issue 3, 1998, Pages 306-310

  Glynn, Susan L ^a   Yazdanian, Mehran ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIRETROVIRUS AGENT; DELAVIRDINE; DIDANOSINE; INDINAVIR; NEVIRAPINE; RNA DIRECTED DNA POLYMERASE INHIBITOR; SAQUINAVIR; STAVUDINE; ZALCITABINE; ZIDOVUDINE;

ANIMAL CELL; ANTIVIRAL ACTIVITY; ARTICLE; BLOOD BRAIN BARRIER; BRAIN BLOOD VESSEL; DRUG PENETRATION; ENDOTHELIUM CELL; ENZYME INHIBITION; HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MEMBRANE PERMEABILITY; NONHUMAN; VIRUS REPLICATION;

EID: 0031946993     PISSN: 00223549     EISSN: None     Source Type: Journal    
DOI: 10.1021/js970291i     Document Type: Article

References (27)

1. Pang, S.; Koyangi, Y.; Miles, S.; Wiley: C.; Harry, V.; Chen, I. High levels of unintegrated HIV-1 DNA in brain tissue of AIDS dementia patients. Nature 1990, 34, 85-89.
2. Spencer, D. C.; Price, R. W. Human Immunodeficiency Virus and the Central Nervous System. Annu. Rec. Microbiol. 1992, 46, 655-693.
3. Lipton, S. A.; Gendelman, H. E. Dementia associated with the acquired immunodeficiency syndrome. N. Engl. J. Med. 1995, 332, 934-940.
4. Hurwitz, A. A.; Berman, J. W.; Lyman, W. D.. The role of the blood brain barrier in HIV infection of the central nervous system. Adv. Neuroimmuno. 1994, 4, 249-256.
5. Bowman, P. D.; Ennis, S. R.; Rarey, K. E.; Betz, A. L.; Goldstein, G. W. Brain microvessel endothelial cells in tissue culture: A model for study of blood-brain barrier permeability. Ann. Neurol. 1983, 14, 396-402.
6. Audus, K. A.; Borchardt, R. T. Characterization of an in vitro blood-brain barrier model system for studying drug transport and metabolism. Pharm. Res, 1986, 3, 81-87.
7. Cserr, H. F.; Bindgaard, M. Blood-brain interfaces in vertebrates: a comparative approach. Am. J. Physiol. 1984, 246, R277-R288.
8. Audus, K. A.; Bartel, R. L.; Hidalgo I. J.; Borchardt, R. T. The use of cultured epithelial and endothelial cells for drug transport and metabolism studies. Pharm. Res. 1990, 7, 435-451.
9. Méresse, S.; Dehouck, M.-P.; Delorme, P.; Bensaïd, M.; Tauber, J.-P.; Delbart, C.; Fruchart, J.-C.; Ceccelli, R. Bovine brain endothelial cells express tight junctions and monoamine oxidase activity in long-term culture. J. Neuorchem. 1989, 53, 1363-1371.
10. Audus, K. A.; Borchardt, R. T. Bovine brain microvessel endothelial cell monolayers as a model system for the blood-brain-barrier. Ann. N.Y. Acad. Sci. 1987, 507, 9-18.
11. Ho, N. F. H.; Park, J. Y.; Ni, P. F.; Higuchi, W. I. Advancing quatitative and mechanistic approaches in interfacing gastrointestinal drug absorption studies in animals and man. In Animal Models for Oral Drug Delivery in Man: In Situ and In Vivo Approaches; Crouthamel, W. G., Sarapu, A., Eds.; APhA/APS, Washington, DC, 1983; pp 27-106.
12. Cheung, A. P.; Kenney, D. Partition coefficients and capacity factors of some nucleoside analogues. J. Chrom. 1990, 506, 119-131.
13. Masereeuw, R.; Jaehde, U.; Langemeijer, M. W. E.; de Boer, A. G.; Breimer, D. D. In vitro and in vivo transport of zidovudine (AZT) across the blood-brain barrier and the effect of transport inhibitors. Pharm. Res. 1994, 11, 324-330.
14. Invirase, Saquinavir mesylate, Roche Laboratories Inc. Package Insert.
15. Lin, J. H.; Chiba., M.; Balani, S. K.; Chen, I.; Kwei, G. Y. S.; Vastag, K. J.; Nishime, J. A. Species differences in the pharmacokinetics and metabolism of indinavir, a potent human immunodeficiency virus inhibitor. Drug. Metab. Dispos. 1996, 24, 1111-1120.
16. Oldendorf, W. H. Lipid solubility and drug penetration of the blood brain barrier. Proc. Soc. Exp. Biol. Med. 1974, 147, 813-816.
17. Levin, V. A. Relationship of octanol/water partition coefficient and molecular weight to rat brain capillary permeability. J. Med. Chem. 1980, 23, 682-684.
18. Shah, M. V.; Audus, K. A.; Borchardt, R. T. The application of bovine brain mic rovessel endothelial cell monolayers grown onto polycarbonate membranes in vitro to estimate the potential permeability of solutes through the blood-brain barrier. Pharm. Res. 1989, 6, 624-627.
19. Barrand, M. A., Robertson, K. J., von Wiekersthal, S. F. Comparisons of P-glycoprotein in isolated rat brain microvessels and in primary cultures of endothelial cells derived from microvasculature of rat brain, epididymal fat pad and from aorta. FEBS Lett. 1995, 374, 179-183.
20. Shelton, M. J.; O'Donnell, A. M.; Morse, G. D. Didanosine. Ann. Pharmacother. 1992, 26, 660-670.
21. Anderson, B. D.; Hoesterey, B. L.; Baker, D. C.; Galinsky, R. E. Uptake kinetics of 2′,3′-dideoxyinosine into brain and cerebrospinal fluid of rats: intravenous infusion studies. J. Pharmacol. Exp. Ther. 1990, 253, 113-118.
22. Murphy, R.; Montaner, J. Nevirapine: A review of its development, pharmacological profile and potential clinical use. Exp. Opin. Invest. Drugs 1996, 5, 1183-1199.
23. Silverstein, H.; Riska, P.; Johnstone, J. N.; Richter, I.; Norris, S.; Hattox, S.; Grob. P. Nevirapine, a Nonnucleoside Reverse Transeriptase Inhibitor, Freely Enters the Brain and crosses the Placental Barrier. XI International Conference on AIDS, Vancouver British Columbia, Canada, July 9, 1996, Abstract 2325.
24. Zerit, Stavudine, Bristol Meyers Squibb. Package Insert.
25. Yarchoan, R.; Perno, C. F.; Thomas, R. V.; Klecker, R. W.; Allain, J-P.; Wills, R. J.; McAtee, N.; Fischl, M. A.; Dubinsky, R.; McNeely, M. C.; Mitsuya, H.; Pluda, J. M.; Lawley, T. J.; Leuther, M.; Safai, B.; Colllins, J. M.; Myers, C. E.; Border. S. Phase I studies of 2′,3′-dideoxycitidine in severe human immunodeficiency virus infection as a single agent and alternating with zidovudine (AZT). Lancet 1988, 1 (8577), 76-81.
26. Klecker, R. W.; Collins, J. M.; Yarchoan, R.; Thomas, R.; Jenkins, J. F.; Border, S.; Myers, C. E. Plasma and cerebrospinal fluid pharmacokinetics of 3′-azido-3′-deoxythymidine: A novel pyrimidine analogue with potential applications for the treatment of patients with AIDS and related diseases. Clin. Pharmacol. Ther. 1987, 41, 407-412.
27. Ståhle, L.; Guzenda, E.; Ljungdahle-Ståhle, E. Pharmacokinetics and extracellular distribution to blood, brain, and muscle of alovudine (3′-fluorothymidine) and zidovudine in the rat studied by microdialysis. J. Accquir. Immune Deffic. Syndr. 1993, 6, 435-439.