Nanoparticles as drug delivery agents specific for CNS: in vivo biodistribution

The pharmacological treatment of neurological disorders is often complicated by the inability of drugs to pass the Blood Brain Barrier. Recently we discovered that polymeric nanoparticles (Np) made of poly(D,L-lactide-co-glycolide) surface-decorated with the peptide Gly-L-Phe-D-Thr-Gly-L-Phe-L-Leu-L-Ser(O--D-Glucose)-CONH2 are able to deliver, after i.v. administration, the model drug loperamide into Central Nervous System (CNS). This new drug delivery agent is able to ensure a strong and long-lasting pharmacological effect, far greater than that previously observed with other nanoparticulate carriers. Here, we confirmed the effectiveness of this carrier for brain targeting comparing the effect obtained by the administration of loperamide-loaded Np with the effect of an intracerebroventricular administration of the drug; moreover, the biodistribution of these Np showed a localization into CNS in a quantity about two orders of magnitude greater than that found with the other known Np drug carriers. Thus, a new kind of Np that target CNS with a very high specificity was discovered