Delivery of Loperamide Across the Blood-Brain Barrier with Polysorbate 80-Coated Polybutylcyanoacrylate Nanoparticles
- 1k Downloads
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.
Unable to display preview. Download preview PDF.
- 1.S. D. Tröster, U. Müller, and J. Kreuter. Int. J. Pharm. 61:85–100 (1990).Google Scholar
- 2.G. Borchard, K. L. Audus, F. Shi and J. Kreuter. Int. J. Pharm. 110:29–35 (1994).Google Scholar
- 3.R. Alyautdin, D. Gothier, V. Petrov, D. Kharkevich, and J. Kreuter. Eur. J. Pharm. Biopharm. 41:44–48 (1995).Google Scholar
- 4.J. Kreuter, R. Alyautdin, D. Kharkevich, and A. Ivanov. Brain Res. 674:171–174 (1995).Google Scholar
- 5.G. Giagnoni, L. Casiraghi, L. Senini, and D. Revel. Life Sci. 33:315–318 (1983).Google Scholar
- 6.C. J. E. Niemegeers, F. M. Lenaerts, and P. A. Janssen. Arzneim. Forsch. (Drug Res.) 24:1633–1653 (1974).Google Scholar
- 7.J. Kreuter. Pharm. Acta Helv. 58:196–209 (1983).Google Scholar
- 8.P. H. Beck, J. Kreuter, E. G. Müller, and W. Schatton. Eur. J. Pharm. Biopharm. 40:134–137 (1994).Google Scholar
- 9.J. Kreuter. Int. J. Pharm. 14:43–58 (1983).Google Scholar
- 10.R. H. Müller, C. Lherm, J. Herbort, T. Blunk, and P. Couvreur. Int. J. Pharm. 84:1–11 (1992).Google Scholar
- 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.M. N. Azmin, J. F. Stuart, K. C. Calman, and A. T. Florence. Cancer Chemother. Pharmacol. 9:161–164 (1982).Google Scholar
- 13.M. N. Azmin, J. F. Stuart, and A. T. Florence. Cancer Chemother. Pharmacol. 14:238–242 (1985).Google Scholar
- 14.C. J. H. Porter, S. M. Moghimi, L. Illum, and S. S. Davis. FEBS Letters. 305:62–66 (1992).Google Scholar
- 15.S. M. Moghimi, and H. M. Patel. Biochim. Biophys. Acta. 948:379–383 (1989).Google Scholar
- 16.T. Blunk, D. F. Hochstrasser, J.-C. Sanchez, B. W. Müller, and R. H. Müller. Electrophoresis. 14:1382–1387 (1993).Google Scholar