Role of Monocarboxylate Transporters in Drug Delivery to the Brain

Vijay, Nisha; Morris, Marilyn

doi:10.2174/13816128113199990462

Cited by 408Drug Transport and Resistance MechanismsBarrier Structure and Function StudiesAmino Acid Enzymes and Metabolism

Role of Monocarboxylate Transporters in Drug Delivery to the Brain

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Vijay, Nisha, Morris, Marilyn·2014·Current Pharmaceutical Design

DOI 10.2174/13816128113199990462PMC PMC4084603

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Abstract

Monocarboxylate transporters (MCTs) are known to mediate the transport of short chain monocarboxylates such as lactate, pyruvate and butyrate. Currently, fourteen members of this transporter family have been identified by sequence homology, of which only the first four members (MCT1- MCT4) have been shown to mediate the proton-linked transport of monocarboxylates. Another transporter family involved in the transport of endogenous monocarboxylates is the sodium coupled MCTs (SMCTs). These act as a symporter and are dependent on a sodium gradient for their functional activity. MCT1 is the predominant transporter among the MCT isoforms and is present in almost all tissues including kidney, intestine, liver, heart, skeletal muscle and brain. The various isoforms differ in terms of their substrate specificity and tissue localization. Due to the expression of these transporters in the kidney, intestine, and brain, they may play an important role in influencing drug disposition. Apart from endogenous short chain monocarboxylates, they also mediate the transport of exogenous drugs such as salicylic acid, valproic acid, and simvastatin acid. The influence of MCTs on drug pharmacokinetics has been extensively studied for γ-hydroxybutyrate (GHB) including distribution of this drug of abuse into the brain and the results will be summarized in this review. The physiological role of these transporters in the brain and their specific cellular localization within the brain will also be discussed. This review will also focus on utilization of MCTs as potential targets for drug delivery into the brain including their role in the treatment of malignant brain tumors.

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Abundant expression of monocarboxylate transporters in endothelial cells might facilitate crossing of the blood-brain barrier by short-chain fatty acids, since brain uptake of short-chain fatty acids has been demonstrated in rats following injection of 14C-SCFAs into the carotid artery.
“The abundant expression of MCTs in endothelial cells (75, 92) might facilitate crossing of the BBB by SCFAs since brain uptake of SCFAs has previously been demonstrated in rats following injection of 14C-SCFAs into the carotid artery (93).”
From The Role of Short-Chain Fatty Acids From Gut Microbiota in Gut-Brain Communication (2020) · cites this paper as [75]
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SCFAs can cross the BBB via monocarboxylate transporters (MCTs) on endothelial cells.
“In vitro studies have shown that SCFAs can cross the BBB via monocarboxylate transporters (MCTs) on endothelial cells (Mitchell et al., 2011; Vijay & Morris, 2014).”
From The modulatory effects of gut microbes and metabolites on blood-brain barrier integrity and brain function in sepsis-associated encephalopathy (2023) · cites this paper as Vijay & Morris, 2014
SCFAs maintain blood-brain barrier integrity through tight-junction protein regulation, as demonstrated in germ-free mice.
“SCFAs also maintain blood–brain barrier (BBB) integrity through tight-junction protein regulation, as demonstrated in studies with germ-free mice [94,95,96].”
From Unraveling the Connections: Eating Issues, Microbiome, and Gastrointestinal Symptoms in Autism Spectrum Disorder (2025) · cites this paper as [94]
SCFA receptors, mainly free fatty acid receptors and monocarboxylate transporters, have been discovered in the central and peripheral nervous systems, indicating direct signaling potential.
“Importantly, SCFA receptors, mainly free fatty acid receptors (349) and monocarboxylate transporters (350, 351), have been discovered in the central nervous system (CNS) and peripheral nervous system, indicating direct signaling potential.”
From Diet and the Microbiota–Gut–Brain Axis: Sowing the Seeds of Good Mental Health (2021) · cites this paper as [350]

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[21]Wilson MC Meredith D Fox JE Manoharan C Davies AJ Halestrap AP Basigin (CD147) is the target for organomercurial inhibition of monocarboxylate transporter isoforms 1 and 4: the ancillary protein for the insensitive MCT2 is EMBIGIN (gp70) J Biol Chem 2005 280 27213 21 15917240
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Authors: Vijay, N., & Morris, M.
Affiliations: University at Buffalo, State University of New York (US)
ORCID: Morris, Marilyn
Venue: Current Pharmaceutical Design
Publisher: Bentham Science Publishers Ltd.
Published: 2014-03-31
Volume: 20
Issue: 10
Pages: 1487-1498
ISSN: 1381-6128 (ISSN-L)
DOI: 10.2174/13816128113199990462
PMC: PMC4084603
OpenAlex: W2043175749
Cited by: 408
References: 121
Citations by year: 2026: 28 · 2025: 41 · 2024: 69 · 2023: 65 · 2022: 47 · 2021: 51 · 2020: 33 · 2019: 18 · 2018: 14 · 2017: 13 · 2016: 17 · 2015: 3 · 2014: 8 · 2013: 1
FWCI: 6.60
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Locations: Current Pharmaceutical Design (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: National Institute on Drug Abuse (DA 023223, R01DA023223)
Topics: Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Life Sciences › Neuroscience › Neurology › Barrier Structure and Function Studies
Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Amino Acid Enzymes and Metabolism
Keywords: monocarboxylate transporters, MCT1, MCT4, brain drug delivery, lactate transport, pyruvate transport, pharmacokinetics, gamma-hydroxybutyric acid, drug disposition, brain tumor therapy, transporter isoforms
MeSH terms: Animals, Blood-Brain Barrier, Brain, Pharmaceutical Preparations, Humans, Drug Delivery Systems, Monocarboxylic Acid Transporters

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Role of Monocarboxylate Transporters in Drug Delivery to the Brain

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