Next Article in Journal
Application of Upstream Open Reading Frames (uORFs) Editing for the Development of Stress-Tolerant Crops
Next Article in Special Issue
Blood–Brain Barrier and Neurovascular Unit In Vitro Models for Studying Mitochondria-Driven Molecular Mechanisms of Neurodegeneration
Previous Article in Journal
RAD51 Inhibition Induces R-Loop Formation in Early G1 Phase of the Cell Cycle
Previous Article in Special Issue
SSAO/VAP-1 in Cerebrovascular Disorders: A Potential Therapeutic Target for Stroke and Alzheimer’s Disease
Review

Disease-Induced Modulation of Drug Transporters at the Blood–Brain Barrier Level

1
Tabula Rasa HealthCare, Precision Pharmacotherapy Research and Development Institute, Orlando, FL 32827, USA
2
Faculty of Pharmacy, Université de Montréal, Montreal, QC H3C 3J7, Canada
*
Author to whom correspondence should be addressed.
Academic Editor: Ryszard Pluta
Int. J. Mol. Sci. 2021, 22(7), 3742; https://doi.org/10.3390/ijms22073742
Received: 3 February 2021 / Revised: 30 March 2021 / Accepted: 1 April 2021 / Published: 3 April 2021
(This article belongs to the Special Issue The Blood-Brain Barrier in Health and Disease)
The blood–brain barrier (BBB) is a highly selective and restrictive semipermeable network of cells and blood vessel constituents. All components of the neurovascular unit give to the BBB its crucial and protective function, i.e., to regulate homeostasis in the central nervous system (CNS) by removing substances from the endothelial compartment and supplying the brain with nutrients and other endogenous compounds. Many transporters have been identified that play a role in maintaining BBB integrity and homeostasis. As such, the restrictive nature of the BBB provides an obstacle for drug delivery to the CNS. Nevertheless, according to their physicochemical or pharmacological properties, drugs may reach the CNS by passive diffusion or be subjected to putative influx and/or efflux through BBB membrane transporters, allowing or limiting their distribution to the CNS. Drug transporters functionally expressed on various compartments of the BBB involve numerous proteins from either the ATP-binding cassette (ABC) or the solute carrier (SLC) superfamilies. Pathophysiological stressors, age, and age-associated disorders may alter the expression level and functionality of transporter protein elements that modulate drug distribution and accumulation into the brain, namely, drug efficacy and toxicity. This review focuses and sheds light on the influence of inflammatory conditions and diseases such as Alzheimer’s disease, epilepsy, and stroke on the expression and functionality of the BBB drug transporters, the consequential modulation of drug distribution to the brain, and their impact on drug efficacy and toxicity. View Full-Text
Keywords: the blood–brain barrier; drug transporters; Alzheimer’s disease; stroke; epilepsy; neuroinflammation the blood–brain barrier; drug transporters; Alzheimer’s disease; stroke; epilepsy; neuroinflammation
Show Figures

Figure 1

MDPI and ACS Style

Al Rihani, S.B.; Darakjian, L.I.; Deodhar, M.; Dow, P.; Turgeon, J.; Michaud, V. Disease-Induced Modulation of Drug Transporters at the Blood–Brain Barrier Level. Int. J. Mol. Sci. 2021, 22, 3742. https://doi.org/10.3390/ijms22073742

AMA Style

Al Rihani SB, Darakjian LI, Deodhar M, Dow P, Turgeon J, Michaud V. Disease-Induced Modulation of Drug Transporters at the Blood–Brain Barrier Level. International Journal of Molecular Sciences. 2021; 22(7):3742. https://doi.org/10.3390/ijms22073742

Chicago/Turabian Style

Al Rihani, Sweilem B., Lucy I. Darakjian, Malavika Deodhar, Pamela Dow, Jacques Turgeon, and Veronique Michaud. 2021. "Disease-Induced Modulation of Drug Transporters at the Blood–Brain Barrier Level" International Journal of Molecular Sciences 22, no. 7: 3742. https://doi.org/10.3390/ijms22073742

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop