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

Journal of Pharmaceutical Sciences
S L Glynn, M Yazdanian

Abstract

To combat infection and inhibit viral replication of HIV in the brain, antiretroviral agents must cross the blood-brain barrier (BBB). An in vitro BBB model consisting of bovine brain microvessel endothelial cells grown on porous filters was used to study and compare the transport of nevirapine, a potent and selective nonnucleoside reverse transcriptase inhibitor, with other HIV antiretroviral agents currently in use for the treatment of HIV infection. These included nucleoside reverse transcriptase inhibitors (didanosine, stavudine, zalcitabine, zidovudine), a nonnucleoside reverse transcriptase (delaviridine), and protease inhibitors (indinavir, saquinavir, VX-478). Nevirapine was the most permeable antiretroviral agent studied in the BBB model. The order of in vitro BBB permeability was nevirapine > VX-478 > didanosine, stavudine, zalcitabine, zidovudine > indinavir > saquinavir. There was an apparent bell-shaped relationship between in vitro BBB permeability and octanol/phosphate-buffered saline distribution coefficient (D) where all lipophilic (log D > 2.5) as well as hydrophilic (log D < -0.5) antiretrovirals were less permeable than nevirapine (log D = 1.8). There were no significant effects on the in vitro BBB permeabil...Continue Reading

References

May 1, 1992·The Annals of Pharmacotherapy·M J SheltonG D Morse
Jan 1, 1992·Annual Review of Microbiology·D C Spencer, R W Price
May 11, 1990·Journal of Chromatography·A P Cheung, D Kenney
Jan 1, 1987·Annals of the New York Academy of Sciences·K L Audus, R T Borchardt
Dec 1, 1974·Proceedings of the Society for Experimental Biology and Medicine·W H Oldendorf
Jan 1, 1994·Advances in Neuroimmunology·A A HurwitzW D Lyman

❮ Previous
Next ❯

Citations

Dec 7, 2005·Journal of Computer-aided Molecular Design·S R Mente, F Lombardo
Apr 4, 2007·Pharmaceutical Research·Nunzio DenoraGaetano Liso
Jan 22, 2003·Advanced Drug Delivery Reviews·Haiying SunWilliam F Elmquist
Jun 6, 2000·Advanced Drug Delivery Reviews·X Li, W K Chan
Jun 6, 2000·Advanced Drug Delivery Reviews·G C Williams, P J Sinko
Oct 24, 2001·European Journal of Medicinal Chemistry·J A PlattsD Butina
Mar 7, 2001·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·L ZhangL B Sheiner
Dec 16, 2005·Cell Research·J Roberto TrujilloRobert C Gallo
Dec 12, 2001·HIV Medicine·S Taylor, A Pereira
Jun 22, 2000·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·J G Gerber
Oct 29, 2000·AIDS Research and Human Retroviruses·A V AlbrightF González-Scarano
Jun 10, 2004·AIDS Research and Human Retroviruses·Stefan EversIngo-W Husstedt
Jun 22, 1999·AIDS Patient Care and STDs·S SwindellsH E Gendelman
Feb 7, 2001·Sexually Transmitted Infections·S Taylor, A S Pereira
Nov 5, 2002·Annual Review of Pharmacology and Toxicology·A G de BoerP J Gaillard
Dec 12, 2001·Clinical Pharmacokinetics·P F SmithG D Morse
Oct 1, 2010·Therapeutic Delivery·V Mangas-SanjuanM Bermejo
Jul 30, 2014·Journal of Pharmacokinetics and Pharmacodynamics·Manuel IbarraPietro Fagiolino
Jun 19, 2004·Journal of Drug Targeting·Remigijus DidziapetrisAlanas Petrauskas
Jul 9, 2004·Drug Metabolism Reviews·Yaming SuPatrick J Sinko
Jul 26, 2006·Expert Opinion on Drug Metabolism & Toxicology·Qing MaGene D Morse
Jun 26, 2012·Médecine et maladies infectieuses·P DellamonicaR Garraffo
Dec 6, 2011·Colloids and Surfaces. B, Biointerfaces·Yung-Chih Kuo, Chin-Hsun Lu
Jul 18, 2008·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Xu-Chun FuJian-Qing Gao
Jul 18, 2006·British Journal of Clinical Pharmacology·Andrew OwenMunir Pirmohamed

❮ Previous
Next ❯

Related Concepts

Related Feeds

Blood Brain Barrier

The blood brain barrier is a border that separates blood from cerebrospinal fluid. Discover the latest search on this highly selective semipermeable membrane here.

Blood Brain Barrier Chips

The blood brain barrier (BBB) is comprised of endothelial cells that regulate the influx and outflux of plasma concentrations. Lab-on-a-chip devices allow scientists to model diseases and mechanisms such as the passage of therapeutic antibodies across the BBB. Discover the latest research on BBB chips here.

Blood Brain Barrier Regulation in Health & Disease

The blood brain barrier is essential in regulating the movement of molecules and substances in and out of the brain. Disruption to the blood brain barrier and changes in permeability allow pathogens and inflammatory molecules to cross the barrier and may play a part in the pathogenesis of neurodegenerative disorders. Here is the latest research in this field.