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Peptide drug delivery into the central nervous system
1Center for Drug Discovery, College of Pharmacy, University of Florida, J. Hillis Miller Health Center, Gainesville 32610-0497, USA.
Summary
Peptides face significant challenges entering the central nervous system (CNS) due to the blood-brain barrier. This review explores strategies to overcome this barrier for novel peptide-based neuropharmaceuticals.
Area of Science:
- Neuroscience
- Pharmacology
- Biochemistry
Background:
- The central nervous system (CNS) microvasculature forms a continuous lipid bilayer, acting as a blood-brain barrier (BBB).
- This BBB restricts the passage of polar, lipid-insoluble substances, including peptides, due to tight junctions and metabolic enzymes.
- Peptides are generally excluded from the brain and spinal cord, limiting their therapeutic potential for neurological diseases.
Purpose of the Study:
- To critically evaluate methods for overcoming the BBB for peptide delivery.
- To explore the potential of peptides as future neuropharmaceuticals.
Main Methods:
- Review of invasive, chemical-enzymatic (prodrug, chemical delivery/targeting systems), and biological carrier-based approaches.
- Critical evaluation of existing strategies for BBB penetration.
Main Results:
- The BBB poses a significant obstacle to peptide drug delivery to the CNS.
- Various strategies are being investigated to facilitate peptide transport across the BBB.
Conclusions:
- Overcoming the BBB is crucial for utilizing peptides as neuropharmaceuticals.
- Further research into delivery systems is needed to unlock the therapeutic potential of peptides for brain and spinal cord diseases.