Document Type
Article
Publication Date
12-2016
Abstract
Introduction: Desired clinical outcome of pharmacotherapy of brain diseases largely depends upon the safe drug delivery into the brain parenchyma. However, due to the robust blockade function of the blood-brain barrier (BBB), drug transport into the brain is selectively controlled by the BBB formed by brain capillary endothelial cells and supported by astrocytes and pericytes. Methods: In the current study, we have reviewed the most recent literature on the subject to provide an insight upon the role and impacts of BBB on brain drug delivery and targeting. Results: All drugs, either small molecules or macromolecules, designated to treat brain diseases must adequately cross the BBB to provide their therapeutic properties on biological targets within the central nervous system (CNS). However, most of these pharmaceuticals do not sufficiently penetrate into CNS, failing to meet the intended therapeutic outcomes. Most lipophilic drugs capable of penetrating BBB are prone to the efflux functionality of BBB. In contrast, all hydrophilic drugs are facing severe infiltration blockage imposed by the tight cellular junctions of the BBB. Hence, a number of strategies have been devised to improve the efficiency of brain drug delivery and targeted therapy of CNS disorders using multimodal nanosystems (NSs). Conclusions: In order to improve the therapeutic outcomes of CNS drug transfer and targeted delivery, the discriminatory permeability of BBB needs to be taken under control. The carriermediated transport machineries of brain capillary endothelial cells (BCECs) can be exploited for the discovery, development and delivery of small molecules into the brain. Further, the receptormediated transport systems can be recruited for the delivery of macromolecular biologics and multimodal NSs into the brain.
Recommended Citation
Barar, Jaleh; Rafi, Mohammad; Pourseif, Mohamad Mostafa; and Omidi, Yadollah, "Blood-brain barrier transport machineries and targeted therapy of brain diseases" (2016). Department of Neurology Faculty Papers. Paper 127.
https://jdc.jefferson.edu/neurologyfp/127
Creative Commons License
This work is licensed under a Creative Commons Attribution-Noncommercial 4.0 License
Comments
This article has been peer reviewed. It is the author’s final published version in BioImpacts
Volume 6, Issue 4, December 2016, Pages 225-248.
The published version is available at DOI: 10.15171/bi.2016.30. Copyright © Barar et al.