Next Article in Journal
Novel Sustained-Release Drug Delivery System for Dry Eye Therapy by Rebamipide Nanoparticles
Next Article in Special Issue
Cannabinoids, Blood–Brain Barrier, and Brain Disposition
Previous Article in Journal
Endoplasmic Reticulum-Associated Degradation-Dependent Processing in Cross-Presentation and Its Potential for Dendritic Cell Vaccinations: A Review
Previous Article in Special Issue
Targeting Small Molecule Delivery to the Brain and Spinal Cord via Intranasal Administration of Rabies Virus Glycoprotein (RVG29)-Modified PLGA Nanoparticles
Review

Transporter-Mediated Delivery of Small Molecule Drugs to the Brain: A Critical Mechanism That Can Advance Therapeutic Development for Ischemic Stroke

Department of Pharmacology, College of Medicine, University of Arizona, 1501 N. Campbell Avenue, P.O. Box 245050, Tucson, AZ 85724-5050, USA
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(2), 154; https://doi.org/10.3390/pharmaceutics12020154
Received: 31 December 2019 / Revised: 10 February 2020 / Accepted: 11 February 2020 / Published: 14 February 2020
(This article belongs to the Special Issue Drug Delivery to the Brain)
Ischemic stroke is the 5th leading cause of death in the United States. Despite significant improvements in reperfusion therapies, stroke patients still suffer from debilitating neurocognitive deficits. This indicates an essential need to develop novel stroke treatment paradigms. Endogenous uptake transporters expressed at the blood-brain barrier (BBB) provide an excellent opportunity to advance stroke therapy via optimization of small molecule neuroprotective drug delivery to the brain. Examples of such uptake transporters include organic anion transporting polypeptides (OATPs in humans; Oatps in rodents) and organic cation transporters (OCTs in humans; Octs in rodents). Of particular note, small molecule drugs that have neuroprotective properties are known substrates for these transporters and include 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (i.e., statins) for OATPs/Oatps and 1-amino-3,5-dimethyladamantane (i.e., memantine) for OCTs/Octs. Here, we review current knowledge on specific BBB transporters that can be targeted for improvement of ischemic stroke treatment and provide state-of-the-art perspectives on the rationale for considering BBB transport properties during discovery/development of stroke therapeutics. View Full-Text
Keywords: blood-brain barrier; drug delivery; HMG-CoA reductase inhibitors; organic anion transporting polypeptides; neurovascular unit; stroke; transporter blood-brain barrier; drug delivery; HMG-CoA reductase inhibitors; organic anion transporting polypeptides; neurovascular unit; stroke; transporter
Show Figures

Figure 1

MDPI and ACS Style

Williams, E.I.; Betterton, R.D.; Davis, T.P.; Ronaldson, P.T. Transporter-Mediated Delivery of Small Molecule Drugs to the Brain: A Critical Mechanism That Can Advance Therapeutic Development for Ischemic Stroke. Pharmaceutics 2020, 12, 154. https://doi.org/10.3390/pharmaceutics12020154

AMA Style

Williams EI, Betterton RD, Davis TP, Ronaldson PT. Transporter-Mediated Delivery of Small Molecule Drugs to the Brain: A Critical Mechanism That Can Advance Therapeutic Development for Ischemic Stroke. Pharmaceutics. 2020; 12(2):154. https://doi.org/10.3390/pharmaceutics12020154

Chicago/Turabian Style

Williams, Erica I.; Betterton, Robert D.; Davis, Thomas P.; Ronaldson, Patrick T. 2020. "Transporter-Mediated Delivery of Small Molecule Drugs to the Brain: A Critical Mechanism That Can Advance Therapeutic Development for Ischemic Stroke" Pharmaceutics 12, no. 2: 154. https://doi.org/10.3390/pharmaceutics12020154

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
Search more from Scilit
 
Search
Back to TopTop