Journal
PHARMACEUTICS
Volume 13, Issue 5, Pages -Publisher
MDPI
DOI: 10.3390/pharmaceutics13050756
Keywords
pharmacokinetics; blood-brain barrier; brain; magnetic-resonance imaging; preclinical models
Categories
Funding
- National Cancer Institute [F99CA253768-01]
- National Institute of General Medical Sciences [5P20GM121322-03, 5P20GM121322-03S1]
- Mylan Chair Endowment Fund
- METAvivor
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The article discusses the role of blood-brain barrier (BBB) and the determination of K-in values, highlighting their application in various pathological conditions. Furthermore, it compares experimental results with human parallels to validate the data.
The blood-brain barrier (BBB) limits movement of solutes from the lumen of the brain microvascular capillary system into the parenchyma. The unidirectional transfer constant, K-in, is the rate at which transport across the BBB occurs for individual molecules. Single and multiple uptake experiments are available for the determination of K-in for new drug candidates using both intravenous and in situ protocols. Additionally, the single uptake method can be used to determine K-in in heterogeneous pathophysiological conditions such as stroke, brain cancers, and Alzheimer's disease. In this review, we briefly cover the anatomy and physiology of the BBB, discuss the impact of efflux transporters on solute uptake, and provide an overview of the single-timepoint method for determination of K-in values. Lastly, we compare preclinical K-in experimental results with human parallels.
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