Efficacy of oral dalargin-loaded nanoparticle delivery across the blood-brain barrier.

The Leu-enkephalin dalargin normally does not penetrate the blood-brain 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 different 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, our data support the usefulness of nanoparticles as a method to deliver drugs to the brain.