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

The Journal focuses on blood–brain barrier; targeted drug delivery; nano carriers; transcytosis. The blood–brain barrier is a highly selective semipermeable border that separates the circulating blood from the brain and extracellular fluid in the central nervous system (CNS). Drug delivery is the method or process of administering a pharmaceutical compound to achieve a therapeutic effect in humans or animals. For the treatment of human diseases, nasal and pulmonary routes of drug delivery are gaining increasing importance. Targeted drug delivery is a method of delivering medication to a patient in a manner that increases the concentration of the medication in some parts of the body relative to others. A nano carrier is nanomaterial being used as a transport module for a drug. Transcytosis is a type of Transcellular transport in which various macromolecules are transported across the interior of a cell.
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 Nano carrier, across the blood–brain barrier via receptor-mediated transcytosis. Specifically, in this process the Nano carrier–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 Nano carriers, coated with appropriate ligands. Here we briefly discuss brain micro vascular endothelial receptors that have been explored until now, highlighting molecular features that govern the efficiency of Nano carrier-mediated drug delivery into the brain.
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Journal of Pharmaceutical Sciences & Emerging Drugs
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