Cited by 400Barrier Structure and Function StudiesDrug Transport and Resistance MechanismsNanoparticle-Based Drug Delivery

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Targeting Receptor-Mediated Transport for Delivery of Biologics Across the Blood-Brain Barrier

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Lajoie, Jason M., Shusta, Eric V.·2015·Annual Review of Pharmacology and Toxicology

DOI 10.1146/annurev-pharmtox-010814-124852PMC PMC5051266

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Abstract

Biologics are an emerging class of medicines with substantial promise to treat neurological disorders such as Alzheimer's disease, stroke, and multiple sclerosis. However, the blood-brain barrier (BBB) presents a formidable obstacle that appreciably limits brain uptake and hence the therapeutic potential of biologics following intravenous administration. One promising strategy for overcoming the BBB to deliver biologics is the targeting of endogenous receptor-mediated transport (RMT) systems that employ vesicular trafficking to transport ligands across the BBB endothelium. If a biologic is modified with an appropriate targeting ligand, it can gain improved access to the brain via RMT. Various RMT-targeting strategies have been developed over the past 20 years, and this review explores exciting recent advances, emphasizing studies that show brain targeting in vivo.

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Authors: Lajoie, J. M., & Shusta, E. V.
Affiliations: University of Wisconsin–Madison (US)
ORCID: Shusta, Eric V.
Venue: Annual Review of Pharmacology and Toxicology
Publisher: Annual Reviews
Published: 2015-01-06
Volume: 55
Issue: 1
Pages: 613-631
ISSN: 0362-1642 (ISSN-L)
1545-4304
DOI: 10.1146/annurev-pharmtox-010814-124852
PMC: PMC5051266
OpenAlex: W2169055592
Cited by: 399
References: 124
Citations by year: 2026: 23 · 2025: 35 · 2024: 43 · 2023: 41 · 2022: 52 · 2021: 49 · 2020: 42 · 2019: 30 · 2018: 36 · 2017: 22 · 2016: 21 · 2015: 5
FWCI: 1.29
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: The Annual Review of Pharmacology and Toxicology (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Funders: National Institutes of Health
National Human Genome Research Institute (T32HG002760)
National Institute of General Medical Sciences (T32GM008349)
National Institute of Neurological Disorders and Stroke (R01NS071513)
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, receptor-mediated transport, biologics, BBB crossing, vesicle trafficking, targeting ligands, neurological disorders, Alzheimer's disease, stroke, multiple sclerosis
MeSH terms: Animals, Biological Products, Biological Transport, Blood-Brain Barrier, Capillary Permeability, Chemistry, Pharmaceutical, Drug Carriers, Humans, Receptors, Cell Surface, Technology, Pharmaceutical

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Targeting Receptor-Mediated Transport for Delivery of Biologics Across the Blood-Brain Barrier

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