The Leu-enkephalin dalargin normally does not penetrate the blood-brai
n barrier (BBB) when given intravenously. To transport dalargin across
the blood-brain barrier, the peptide was adsorbed onto the surface of
poly(butyl)cyanoacrylate nanoparticles and coated with polysorbate 80
. After systemic administration the central analgesia was measured by
hot plate test. Furthermore, nanoparticles were fabricated with differ
ent stabilizers. After the adsorption of the peptide on polysorbate 85
stabilized nanoparticles analgesia was observable after intravenously
and oral application even when nanoparticles were not coated. Thus, o
ur data support the usefulness of nanoparticles as a method to deliver
drugs to the brain. (C) 1998 Elsevier Science Inc.