Drug delivery to the CNS and polymeric nanoparticulate carriers

Abstract

The delivery of drugs to the CNS is hampered by the existence of the blood–brain barrier (BBB). Nowadays, medicinal chemists follow defined rules for the development of drugs able to cross the BBB. At the same time, the parameters needed in order to gain valuable estimates of brain drug delivery are well defined. Despite the limits in molecular weight that allow drugs to cross the BBB, it was shown that nanotech products, in particular properly functionalized nanoparticles, spherical particles of approximately 200 nm in diameter, are able to cross the BBB after intravenous administration and act as drug carriers for CNS. Moreover, peptides as ligands for receptors present on the brain endothelium, or able to cross the BBB and to act as carriers for CNS drug delivery in the form of conjugates with drugs, have been discovered and started to be studied as targeting moieties for nanoparticulate systems. This article will discuss the results obtained so far in the field of nanoparticle drug carriers for CNS and highlight the parameters needed in order to fully characterize these hitherto largely unknown delivery systems. Even if promising results have been obtained, more studies are needed in order to fully evaluate the clinical potential of this drug-delivery system.