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Smuggling Drugs into the Brain: An Overview of Ligands Targeting Transcytosis for Drug Delivery across the Blood–Brain Barrier

Department of Cell Biology, University Medical Center Groningen, University of Groningen, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands
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Pharmaceutics 2014, 6(4), 557-583; https://doi.org/10.3390/pharmaceutics6040557
Received: 24 September 2014 / Revised: 28 October 2014 / Accepted: 29 October 2014 / Published: 17 November 2014
(This article belongs to the Special Issue Drug Delivery to Brain)
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. View Full-Text
Keywords: blood–brain barrier; targeted drug delivery; nanocarriers; transcytosis blood–brain barrier; targeted drug delivery; nanocarriers; transcytosis
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MDPI and ACS Style

Georgieva, J.V.; Hoekstra, D.; Zuhorn, I.S. Smuggling Drugs into the Brain: An Overview of Ligands Targeting Transcytosis for Drug Delivery across the Blood–Brain Barrier. Pharmaceutics 2014, 6, 557-583. https://doi.org/10.3390/pharmaceutics6040557

AMA Style

Georgieva JV, Hoekstra D, Zuhorn IS. Smuggling Drugs into the Brain: An Overview of Ligands Targeting Transcytosis for Drug Delivery across the Blood–Brain Barrier. Pharmaceutics. 2014; 6(4):557-583. https://doi.org/10.3390/pharmaceutics6040557

Chicago/Turabian Style

Georgieva, Julia V.; Hoekstra, Dick; Zuhorn, Inge S. 2014. "Smuggling Drugs into the Brain: An Overview of Ligands Targeting Transcytosis for Drug Delivery across the Blood–Brain Barrier" Pharmaceutics 6, no. 4: 557-583. https://doi.org/10.3390/pharmaceutics6040557

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