Smuggling Drugs into the Brain: An Overview of Ligands Targeting... (2015)

Whenever we do find drugs to deliver, we will need this.
Smuggling Drugs into the Brain: An Overview of Ligands Targeting... (2015)

Published inPharmaceutics, Vol. 6, No. 4, p.557-83. AuthorZuhorn, Inge; Georgieva, Julia V.; Hoekstra, Dick PublisherCenter for Liver, Digestive and Metabolic Diseases (CLDM); Nanobiotechnology and Advanced Therapeutic Materials (NANOBIOMAT); Molecular Neuroscience and Ageing Research (MOLAR) Date2015 LanguageEnglish TypeArticle 

Abstract

The blood-brain barrier acts as a physical barrier that prevents free entry of blood-derived substances, including those intended for therapeutic applications. The development of molecular Trojan horses is a promising drug targeting technology that allows for non-invasive delivery of therapeutics into the brain. This concept relies on the application of natural or genetically engineered proteins or small peptides, capable of specifically ferrying a drug-payload that is either directly coupled or encapsulated in an appropriate nanocarrier, across the blood-brain barrier via receptor-mediated transcytosis. Specifically, in this process the nanocarrier-drug system ("Trojan horse complex") is transported transcellularly across the brain endothelium, from the blood to the brain interface, essentially trailed by a native receptor. Naturally, only certain properties would favor a receptor to serve as a transporter for nanocarriers, coated with appropriate ligands. Here we briefly discuss brain microvascular endothelial receptors that have been explored until now, highlighting molecular features that govern the efficiency of nanocarrier-mediated drug delivery into the brain. Publicationhttps://www.rug.nl/research/portal/en/publications/smuggling...