Application of nanoparticles for the delivery of drugs to the brain

The mechanism of the drug transport across the blood-brain barrier with the nanoparticles appears to be endocytotic uptake by the brain capillary endothelial cells followed either by release of the drugs in these cells and diffusion into the brain or by transcytosis. After injection of the nanoparticles, apolipoprotein E (apo E) or apo B adsorb on the particle surface and then seem to promote the interaction with the LDL receptor followed by endocytotic uptake. The nanoparticles thus would mimic the uptake of naturally occurring lipoprotein particles. This hypothesis was supported by the achievement of an antinociceptive effect using dalargin-loaded poly(butyl cyanoacrylate) nanoparticles with adsorbed apo E or loperamide-loaded albumin nanoparticles with covalently bound apo E.