Abstract
The blood-brain barrier (BBB), a dynamic and complex barrier formed by endothelial cells, can impede the entry of unwanted substances - pathogens and therapeutic molecules alike - into the central nervous system (CNS) from the blood circulation. Taking into account the fact that CNS-related diseases are the largest and fastest growing unmet medical concern, many potential protein- and nucleic acid-based medicines have been developed for therapeutic purposes. However, due to their poor ability to cross the BBB and the plasma membrane, the above-mentioned bio-macromolecules have limited use in treating neurological diseases. Finding effective, safe, and convenient ways to deliver therapeutic molecules into the CNS is thus urgently required. In recent decades, much effort has been expended in the development of drug delivery technologies, of which cell-penetrating peptides (CPPs) have the most promising potential. The present review covers the latest advances in CPP delivery technology, and provides an update on their use in CNS-targeted drug delivery.
Highlights
The blood-brain barrier (BBB) is a dynamic and complex barrier that exists in all vertebrate organisms with welldeveloped central nervous systems (CNSs) and which is interposed between the blood and CNS to protect the brain against invading pathogenic organisms [1, 2]
Compared with the majority of delivery systems that suffer from various limitations when applied in clinical situations to the transport of therapeutic molecules into the CNS, cell-penetrating peptide (CPP)-based delivery systems show a great ability in carrying macromolecules across cellular membranes, combining a low cellular toxicity with high efficiency [55]
CPPs, which are an attractive type of therapeutic molecule delivery vehicle due to their low toxicity and the wide variety of cell types that they are capable of targeting, represent a potentially valuable tool for the intracellular delivery of therapeutic molecules to alter intracellular signaling pathways as well as interfere with intracellular interactions to rebalance a perturbed cellular function and protect neurons in cases of ischemia and neurodegenerative diseases
Summary
The blood-brain barrier (BBB) is a dynamic and complex barrier that exists in all vertebrate organisms with welldeveloped central nervous systems (CNSs) and which is interposed between the blood and CNS to protect the brain against invading pathogenic organisms [1, 2]. Compared with the majority of delivery systems that suffer from various limitations when applied in clinical situations to the transport of therapeutic molecules into the CNS, cell-penetrating peptide (CPP)-based delivery systems show a great ability in carrying macromolecules across cellular membranes, combining a low cellular toxicity with high efficiency [55]. Considering their smaller size (up to 30 amino acids in length), cationic and/or amphipathic CPPs have a greater potential to penetrate the BBB than other transport systems, enabling them to be used as very promising tools for therapeutic purposes in CNS-related diseases [56].
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