Routes for drug translocation across the blood-brain barrier: Exploiting peptides as delivery vectors

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A number of potent drugs for the treatment of brain diseases are available. However, in order for them to reach their target site of action, they must pass the blood-brain barrier (BBB). The capillary endothelium comprises the major barrier of the BBB and allows only passive permeation of some small lipophilic molecules. Brain delivery of the larger biopharmaceuticals, which today includes an increasing number of novel drug entities, is therefore restricted; both due to their molecular size and their hydrophilic nature. Thus, the development of novel drug entities intended for the treatment of brain diseases such as neurodegenerative diseases or brain cancers, require a delivery strategy for overcoming the BBB before reaching its final target within the brain. Peptide-based delivery vectors is an emerging tool as shuttles for drug delivery across the BBB and one may explore receptor-mediated transcytosis, adsorptive-mediated transcytosis, and the paracellular route. The latter, however, being controversial due to the risk of co-delivery of blood-borne potential harmful substances. On the other hand a number of studies report on drug delivery across the BBB exploiting receptor-mediated transcytosis and adsorptive-mediated transcytosis, indicating that peptides and peptide vectors may be of use in a central nervous system (CNS) delivery context.

Original languageEnglish
JournalJournal of Pharmaceutical Sciences
Issue number9
Pages (from-to)2326-2334
Publication statusPublished - Sep 2017

    Research areas

  • Journal Article, Review

ID: 180851026