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


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 


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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

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