Peptide delivery into the central nervous system: Invasive, physiological and chemical approaches

Research output: Contribution to journalReview article

7 Citations (Scopus)

Abstract

The capillary endothelium of the brain and spinal cord possesses tight junctions and, thus, behaves as a continuous lipid bilayer that prevents the passage of highly polar and lipid-insoluble substances. Highly active enzymes expressed in the brain endothelial cells and cerebral pericytes also represent a metabolic component that contributes to the homeostatic balance of the central nervous system (CNS). Peptides cannot enter the brain and spinal cord from the circulating blood because they are highly polar and lipid insoluble, metabolically unstable, and generally do not have active transport systems in this membranous barrier. Hence, the blood-brain barrier (BBB) is the major obstacle to peptide-based therapeutics that are potentially useful for combating diseases affecting the central nervous system. The article discusses invasive, physiological-based and chemical-enzymatic approaches to overcome the BBB by reviewing both primary and patent literature.

Original languageEnglish
Pages (from-to)233-245
Number of pages13
JournalExpert Opinion on Therapeutic Patents
Volume7
Issue number3
DOIs
StatePublished - 10 Apr 1997

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brain
Central Nervous System
Blood-Brain Barrier
Peptides
Spinal Cord
Brain
Literature
Lipids
Pericytes
Patents
Tight Junctions
Active Biological Transport
Central Nervous System Diseases
Vascular Endothelium
Lipid Bilayers
Fetal Blood
Endothelial Cells
transport system
patent
Enzymes

Cite this

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abstract = "The capillary endothelium of the brain and spinal cord possesses tight junctions and, thus, behaves as a continuous lipid bilayer that prevents the passage of highly polar and lipid-insoluble substances. Highly active enzymes expressed in the brain endothelial cells and cerebral pericytes also represent a metabolic component that contributes to the homeostatic balance of the central nervous system (CNS). Peptides cannot enter the brain and spinal cord from the circulating blood because they are highly polar and lipid insoluble, metabolically unstable, and generally do not have active transport systems in this membranous barrier. Hence, the blood-brain barrier (BBB) is the major obstacle to peptide-based therapeutics that are potentially useful for combating diseases affecting the central nervous system. The article discusses invasive, physiological-based and chemical-enzymatic approaches to overcome the BBB by reviewing both primary and patent literature.",
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Peptide delivery into the central nervous system : Invasive, physiological and chemical approaches. / Prokai, Laszlo.

In: Expert Opinion on Therapeutic Patents, Vol. 7, No. 3, 10.04.1997, p. 233-245.

Research output: Contribution to journalReview article

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