Drug Delivery to the Brain by Liposomal Carrier Systems

Abstract

Endothelial cells of brain microvessels limit the entry into the brain for xenobiotics and many drugs, which otherwise may be therapeutically active in the central nervous system. The ABC transporters, P-glycoprotein and Breast cancer resistance protein, which are predominantly located in the luminal surface of capillary endothelial cells, are key players for this barrier function. Thus, particular efforts have been made to overcome the blood-brain barrier or to circumvent these efflux pumps. The various options for drug transport into the brain include encapsulation of active compounds into delivery systems, e.g. liposomes, which are able to by-pass the export pumps and to convey their payload across the endothelial barrier. The applied systems target receptors at the luminal surface of the blood-brain barrier by using antibodycoupled immunoliposomes, liposomes conjugated to receptor-targeting vectors such as insulin, transferrin and apolipoproteins or cationized albumin-coupled liposomes.

Keywords: Albumin, ApoE, Blood-brain barrier, Immunoliposomes, Insulin, Pglycoprotein, Transferrin.

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