Crossing the Blood–Brain Barrier: Recent Advances in Drug Delivery to the Brain
Abstract
CNS disorders are on the rise despite advancements in our understanding of their pathophysiological mechanisms. A major hurdle to the treatment of these disorders is the blood-brain barrier (BBB), which serves as an arduous janitor to protect the brain. Many drugs are being discovered for CNS disorders, which, however fail to enter the market because of their inability to cross the BBB. This is a pronounced challenge for the pharmaceutical fraternity. Hence, in addition to the discovery of novel entities and drug candidates, scientists are also developing new formulations of existing drugs for brain targeting. Several approaches have been investigated to allow therapeutics to cross the BBB. As the molecular structure of the BBB is better elucidated, several key approaches for brain targeting include physiological transport mechanisms such as adsorptive-mediated transcytosis, inhibition of active efflux pumps, receptor-mediated transport, cell-mediated endocytosis, and the use of peptide vectors. Drug-delivery approaches comprise delivery from microspheres, biodegradable wafers, and colloidal drug-carrier systems (e.g., liposomes, nanoparticles, nanogels, dendrimers, micelles, nanoemulsions, polymersomes, exosomes, and quantum dots). The current review discusses the latest advancements in these approaches, with a major focus on articles published in 2015 and 2016. In addition, we also cover the alternative delivery routes, such as intranasal and convection-enhanced diffusion m…
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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 [6]
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 [6]
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- Authors
- Patel, M. M., & Patel, B. M.
- Affiliations
- Nirma University (IN)
- Corresponding author
- Patel, Mayur M.
- Venue
- CNS Drugs
- Published
- 2017-01-18
- Volume
- 31
- Issue
- 2
- Pages
- 109-133
- ISSN
- 1172-7047 (ISSN-L)
- 1179-1934
- OpenAlex
- W2578392051
- Cited by
- 430
- References
- 6
- Citations by year
- 2026: 28 · 2025: 49 · 2024: 42 · 2023: 57 · 2022: 62 · 2021: 58 · 2020: 56 · 2019: 42 · 2018: 25 · 2017: 11
- FWCI
- 18.06
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- CNS Drugs (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, brain drug delivery, central nervous system disorders, transcytosis, efflux pump inhibition, receptor-mediated transport, endocytosis, peptide vectors, liposomes, nanoparticles, nanogels, dendrimers, micelles, nanoemulsions, polymersomes, exosomes, quantum dots, intranasal drug delivery, blood-brain barrier disruption
- MeSH terms
- Animals, Biological Transport, Blood-Brain Barrier, Brain, Central Nervous System Diseases, Drug Carriers, Humans, Tissue Distribution, Drug Design, Drug Delivery Systems
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