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Current Strategies to Enhance Delivery of Drugs across the Blood–Brain Barrier
Open accessAbstract
The blood–brain barrier (BBB) has shown to be a significant obstacle to brain medication delivery. The BBB in a healthy brain is a diffusion barrier that prevents most substances from passing from the blood to the brain; only tiny molecules can pass across the BBB. The BBB is disturbed in specific pathological illnesses such as stroke, diabetes, seizures, multiple sclerosis, Parkinson’s disease, and Alzheimer’s disease. The goal of this study is to offer a general overview of current brain medication delivery techniques and associated topics from the last five years. It is anticipated that this review will stimulate readers to look into new ways to deliver medications to the brain. Following an introduction of the construction and function of the BBB in both healthy and pathological conditions, this review revisits certain contested questions, such as whether nanoparticles may cross the BBB on their own and if medications are selectively delivered to the brain by deliberately targeted nanoparticles. Current non-nanoparticle options are also discussed, including drug delivery via the permeable BBB under pathological circumstances and the use of non-invasive approaches to improve brain medication absorption.
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![Figure 1 The blood–brain barrier elements. Reprinted from Ref. [14], MDPI, 2021.](/paper-figures/001121684e2b4351b1d28ec51fe7787f/current-strategies-to-enhance-delivery-of-drugs-across-the-bloodbrain-barrier-figure-1.jpg)
![Figure 2 Schematic illustration summarizing some of the major neurological disorders associated with impairment of the BBB. Reprinted from Ref. [25], MDPI, 2021.](/paper-figures/c636fefd8f304253b999e20610081d9d/current-strategies-to-enhance-delivery-of-drugs-across-the-bloodbrain-barrier-figure-2.jpg)
![Figure 3 Schematic representation of cerebral capillary showing endothelial cell in (A) normal and (B) glioblastoma. Reprinted with permission from Ref. [32], Copyright 2020, Elsevier.](/paper-figures/e0d71841fa674a0cb460ad66ecc78d77/current-strategies-to-enhance-delivery-of-drugs-across-the-bloodbrain-barrier-figure-3.jpg)
![Figure 4 Schematic representation of the MRI-guided FUS system used by Park et al. Reprinted from Ref. [138], PLOS, 2017.](/paper-figures/5bfc687f86104b2080e3a92931d21d46/current-strategies-to-enhance-delivery-of-drugs-across-the-bloodbrain-barrier-figure-4.jpg)
![Figure 5 Schematic representation of dual-functionalized (Tf–Pen) liposomes translocation across the BBB, followed by endocytosis into glioblastoma cells. Reprinted with permission from Ref. [173], Copyright 2019, Elsevier.](/paper-figures/bbbe0befc528446cb60dc2aa707b0656/current-strategies-to-enhance-delivery-of-drugs-across-the-bloodbrain-barrier-figure-5.jpg)
![Figure 6 Main BBB crossing pathways for nanosystems. Abbreviations: CNS–central nervous system; NCL–nanostructured lipid carriers; NPs–nanoparticles. Reprinted from Ref. [188], Dove Press Ltd., 2015.](/paper-figures/b601fe915af4476ea279618d1eb45a11/current-strategies-to-enhance-delivery-of-drugs-across-the-bloodbrain-barrier-figure-6.jpg)
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“Another challenge in AD treatments is the efficient delivery and targeting of molecules of interest to the brain due to the protective barriers of the central nervous system [27,28].”
From Alzheimer's Disease: Treatment Strategies and Their Limitations. (2022) · cites this paper as [28]
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Metadata
- Authors
- Teleanu, R. I., Preda, M. D., Niculescu, A.-G., Vladâcenco, O., Radu, C. I., Grumezescu, A. M., & Teleanu, D. M.
- Affiliations
- Carol Davila University of Medicine and Pharmacy (RO)
- Universitatea Națională de Știință și Tehnologie Politehnica București (RO)
- Bucharest Emergency University Hospital (RO)
- University of Bucharest (RO)
- Corresponding author
- Grumezescu, Alexandru Mihai
- ORCID
- Venue
- Pharmaceutics
- Publisher
- MDPI AG
- Published
- 2022-05-04
- Volume
- 14
- Issue
- 5
- Pages
- 987
- ISSN
- 1999-4923 (ISSN-L)
- PMC
- PMC9145636
- OpenAlex
- W4229057365
- Cited by
- 200
- References
- 189
- Citations by year
- 2026: 33 · 2025: 72 · 2024: 57 · 2023: 26 · 2022: 12
- FWCI
- 4.30
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Pharmaceutics (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- 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, nanoparticles, blood-brain barrier disruption, targeted drug delivery, non-invasive drug delivery, blood-brain barrier permeability, neurological disorders, Alzheimer's disease, Parkinson's disease, multiple sclerosis, stroke
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