Skip to main content
SpringerLink
Log in

Carrier-Mediated Transport of Baclofen Across Monolayers of Bovine Brain Endothelial Cells in Primary Culture

  • Published:
Pharmaceutical Research Aims and scope Submit manuscript

Abstract

The mechanism of transport of baclofen, a centrally acting muscle relaxant, across the blood–brain barrier (BBB) was studied using an in vitro model. The model consisted of a monolayer of bovine brain endothelial cells grown in primary culture on a porous regenerated cellulose membrane. The transport of baclofen across the monolayer expressed time and concentration dependency and was saturable. Transport data were corrected for diffusion and fitted to the Michaelis–Menten V max model: K m = 58.5 µM, V max = 0.23 nmol/min. The results validate the use of the in vitro BBB model as described and support the hypothesis that baclofen penetrates the BBB by means of a carrier-mediated transport system.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

REFERENCES

  1. H. A. Fehr, and H. J. Bein. J. Int. Med. Res. 2:36–47 (1974).

    Google Scholar 

  2. N. G. Bowery, D. R. Hill, and A. L. Hudson. Neuropharmacology 24:207–210 (1985).

    Google Scholar 

  3. S. Rim, K. L. Audus, and R. T. Borchardt. Int. J. Pharm. 32:79–84 (1986).

    Google Scholar 

  4. W. H. Oldendorf. Proc. Soc. Exp. Biol. Med. 147:813–816 (1974).

    Google Scholar 

  5. B. B. Brodie, H. Kurz, and L. S. Schanker. J. Pharmacol. Exp. Ther. 130:519–528 (1960).

    Google Scholar 

  6. W. M. Pardridge. In R. T. Borchardt, A. J. Repta, and V. J. Stella, (eds.), Directed Drug Delivery, Humana Press, Clifton, N.J., 1985, pp. 83–96.

    Google Scholar 

  7. K. L. Audus, and R. T. Borchardt. J. Neurochem. 47:484–488 (1986).

    Google Scholar 

  8. K. L. Audus, and R. T. Borchardt. Pharm. Res. 3:81–87 (1986).

    Google Scholar 

  9. A. Baranczyk-Kuzma, K. L. Audus, and R. T. Borchardt. J. Neurochem. 46:1956–1960 (1986).

    Google Scholar 

  10. A. L. Betz, and G. W. Goldstein. Science 202:1580–1583 (1985).

    Google Scholar 

  11. J. T. Hjelle, J. Baird-Lambert, G. Cardinale, S. Spector, and S. Udenfriend. Proc. Natl. Acad. Sci. USA 75:4544–4548 (1978).

    Google Scholar 

  12. D. Bottaro, D. Shepro, S. Peterson, and H. B. Hechtman. J. Cell. Physiol. 128:189–194 (1986).

    Google Scholar 

  13. J. H. Nelder and R. Mead. Comput. J. 7:308–313 (1965).

    Google Scholar 

  14. P. T. Beall, J. Bond, J. Cassidy, K. Rosenweig, and F. H. Clarke Fed. Proc. 44:444 (1985).

    Google Scholar 

  15. W. M. Pardridge and W. H. Oldendorf. Biochim. Biophys. Acta 401:128–136 (1975).

    Google Scholar 

  16. W. M. Pardridge and Th. B. Choi. Fed. Proc. 46:2073–2078 (1986).

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Department of Pharmaceutical Chemistry, The University of Kansas, Lawrence, Kansas, 66045

    Kenneth L. Audus & Ronald T. Borchardt

  2. Center for Bio-Pharmaceutical Sciences, Division of Pharmacology, University of Leiden, P.O.B. 9503, 2300, RA Leiden, The Netherlands

    Joost B. M. M van Bree

Authors
  1. Joost B. M. M van Bree
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Kenneth L. Audus
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Ronald T. Borchardt
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

van Bree, J.B.M.M., Audus, K.L. & Borchardt, R.T. Carrier-Mediated Transport of Baclofen Across Monolayers of Bovine Brain Endothelial Cells in Primary Culture. Pharm Res 5, 369–371 (1988). https://doi.org/10.1023/A:1015959628008

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1023/A:1015959628008

Search

Navigation