Blood–brain barrier delivery
Abstract
Neuropharmaceutics is the largest potential growth sector of the pharmaceutical industry. However, this growth is blocked by the problem of the blood-brain barrier (BBB). Essentially 100% of large-molecule drugs and >98% of small-molecule drugs do not cross the BBB. The BBB can be traversed because there are multiple endogenous transporters within this barrier. Therefore, brain drug development programs of the future need to be re-configured so that drugs are formulated to enable transport into the brain via endogenous BBB transporters.
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Transient blood-brain barrier openings allow leakage of plasma proteins into the brain, leading to neurotoxicity, vascular pathology, and chronic neuropathologic changes.
“Disruption of the BBB, using techniques such as osmotic disruption, biochemical disruption, and ultrasound-mediated disruption, is effective to introduce drugs into the brain; however, these transient BBB openings also allows for the leakage of plasma proteins into the brain, leading to neurotoxicity, vascular pathology, and chronic neuropathologic changes in the brain (1, 7, 11).”
From Neurotransmitter-derived lipidoids (NT-lipidoids) for enhanced brain delivery through intravenous injection (2020) · cites this paper as [1]
Treatment of central nervous system diseases is severely constrained by the blood-brain barrier.
“The treatment of central nervous system (CNS) diseases, such as neurodegenerative disorders, brain tumors, brain infections, and stroke, is severely constrained by the blood-brain barrier (BBB) because it prevents the transfer of most of small-molecule drugs and macromolecules (e.g., peptides, gene drugs, and protein drugs) into the brain (1–6).”
From Neurotransmitter-derived lipidoids (NT-lipidoids) for enhanced brain delivery through intravenous injection (2020) · cites this paper as [1]
Disruption of the blood-brain barrier using osmotic, biochemical, or ultrasound techniques is effective to introduce drugs into the brain.
“Disruption of the BBB, using techniques such as osmotic disruption, biochemical disruption, and ultrasound-mediated disruption, is effective to introduce drugs into the brain; however, these transient BBB openings also allows for the leakage of plasma proteins into the brain, leading to neurotoxicity, vascular pathology, and chronic neuropathologic changes in the brain (1, 7, 11).”
From Neurotransmitter-derived lipidoids (NT-lipidoids) for enhanced brain delivery through intravenous injection (2020) · cites this paper as [1]
The blood-brain barrier prevents the transfer of most small-molecule drugs and macromolecules into the brain.
“it prevents the transfer of most of small-molecule drugs and macromolecules (e.g., peptides, gene drugs, and protein drugs) into the brain (1–6).”
From Neurotransmitter-derived lipidoids (NT-lipidoids) for enhanced brain delivery through intravenous injection (2020) · cites this paper as [1]
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- Authors
- Pardridge, W. M.
- Affiliations
- University of California, Los Angeles (US)
- Corresponding author
- Pardridge, William M.
- Venue
- Drug Discovery Today
- Publisher
- Elsevier BV
- Published
- 2007-01
- Volume
- 12
- Issue
- 1-2
- Pages
- 54-61
- ISSN
- 1359-6446 (ISSN-L)
- OpenAlex
- W1973544766
- Cited by
- 1,191
- References
- 2
- Citations by year
- 2026: 34 · 2025: 51 · 2024: 74 · 2023: 70 · 2022: 67 · 2021: 89 · 2020: 78 · 2019: 57 · 2018: 57 · 2017: 64 · 2016: 67 · 2015: 79 · 2014: 76 · 2013: 73 · 2012: 52
- FWCI
- 2.55
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drug Discovery Today (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Neurology › Barrier Structure and Function Studies
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- blood-brain barrier, neuropharmaceuticals, large molecule drugs, small molecule drugs, drug formulation
- MeSH terms
- Animals, Blood-Brain Barrier, Brain, Pharmaceutical Preparations, Humans, Drug Design, Drug Delivery Systems
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