Pharmaceutical Research

, Volume 14, Issue 3, pp 325–328 | Cite as

Delivery of Loperamide Across the Blood-Brain Barrier with Polysorbate 80-Coated Polybutylcyanoacrylate Nanoparticles

  • Renad N. Alyautdin
  • Valery E. Petrov
  • Klaus Langer
  • Achim Berthold
  • Dimitry A. Kharkevich
  • Jörg Kreuter

Abstract

Purpose. The possibility of using polysorbate 80-coated nanoparticles for the delivery of the water insoluble opioid agonist loperamide across the blood-brain barrier was investigated. The analgesic effect after i.v. injection of the preparations was used to indicate drug transport through this barrier.

Methods. Loperamide was incorporated into PBCA nanoparticles. Drug-containing nanoparticles were coated with polysorbate 80 and injected intravenously into mice. Analgesia was then measured by the tail-flick test.

Results. Intravenous injection of the particulate formulation resulted in a long and significant analgesic effect. A polysorbate 80 loperamide solution induced a much less pronounced and very short analgesia. Uncoated nanoparticles loaded with loperamide were unable to produce analgesia.

Conclusions. Polysorbate 80-coated PBCA nanoparticles loaded with loperamide enabled the transport of loperamide to the brain.

loperamide nanoparticles polysorbate 80 drug delivery brain 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

REFERENCES

  1. 1.
    S. D. Tröster, U. Müller, and J. Kreuter. Int. J. Pharm. 61:85–100 (1990).Google Scholar
  2. 2.
    G. Borchard, K. L. Audus, F. Shi and J. Kreuter. Int. J. Pharm. 110:29–35 (1994).Google Scholar
  3. 3.
    R. Alyautdin, D. Gothier, V. Petrov, D. Kharkevich, and J. Kreuter. Eur. J. Pharm. Biopharm. 41:44–48 (1995).Google Scholar
  4. 4.
    J. Kreuter, R. Alyautdin, D. Kharkevich, and A. Ivanov. Brain Res. 674:171–174 (1995).Google Scholar
  5. 5.
    G. Giagnoni, L. Casiraghi, L. Senini, and D. Revel. Life Sci. 33:315–318 (1983).Google Scholar
  6. 6.
    C. J. E. Niemegeers, F. M. Lenaerts, and P. A. Janssen. Arzneim. Forsch. (Drug Res.) 24:1633–1653 (1974).Google Scholar
  7. 7.
    J. Kreuter. Pharm. Acta Helv. 58:196–209 (1983).Google Scholar
  8. 8.
    P. H. Beck, J. Kreuter, E. G. Müller, and W. Schatton. Eur. J. Pharm. Biopharm. 40:134–137 (1994).Google Scholar
  9. 9.
    J. Kreuter. Int. J. Pharm. 14:43–58 (1983).Google Scholar
  10. 10.
    R. H. Müller, C. Lherm, J. Herbort, T. Blunk, and P. Couvreur. Int. J. Pharm. 84:1–11 (1992).Google Scholar
  11. 11.
    N. De Jaeger, H. Demeyere, R. Finsy, R. Sneyers, J. Vanderdeelen, P. van der Meeren, and M. van Laethem. Part. Part. Syst. Charact. 8:179–186 (1991).Google Scholar
  12. 12.
    M. N. Azmin, J. F. Stuart, K. C. Calman, and A. T. Florence. Cancer Chemother. Pharmacol. 9:161–164 (1982).Google Scholar
  13. 13.
    M. N. Azmin, J. F. Stuart, and A. T. Florence. Cancer Chemother. Pharmacol. 14:238–242 (1985).Google Scholar
  14. 14.
    C. J. H. Porter, S. M. Moghimi, L. Illum, and S. S. Davis. FEBS Letters. 305:62–66 (1992).Google Scholar
  15. 15.
    S. M. Moghimi, and H. M. Patel. Biochim. Biophys. Acta. 948:379–383 (1989).Google Scholar
  16. 16.
    T. Blunk, D. F. Hochstrasser, J.-C. Sanchez, B. W. Müller, and R. H. Müller. Electrophoresis. 14:1382–1387 (1993).Google Scholar

Copyright information

© Plenum Publishing Corporation 1997

Authors and Affiliations

  • Renad N. Alyautdin
    • 1
  • Valery E. Petrov
    • 1
  • Klaus Langer
    • 2
  • Achim Berthold
    • 2
  • Dimitry A. Kharkevich
    • 1
  • Jörg Kreuter
    • 2
  1. 1.Department of PharmacologySechenov Medical AcademyMoscowRussia
  2. 2.Institute of Pharmaceutical TechnologyJohann Wolfgang Goethe-UniversityFrankfurt am MainGermany

Personalised recommendations