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Assessment of brain‐to‐blood drug distribution using liquid chromatography
Author(s) -
El Zahar Noha M.,
Sutton J. Michael,
Bartlett Michael G.
Publication year - 2021
Publication title -
biomedical chromatography
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.4
H-Index - 65
eISSN - 1099-0801
pISSN - 0269-3879
DOI - 10.1002/bmc.5123
Subject(s) - bioanalysis , chemistry , pharmacokinetics , blood–brain barrier , drug , chromatography , pharmacology , distribution (mathematics) , central nervous system , medicine , mathematical analysis , mathematics
Delivery of already existing and new drugs under development to the brain necessitates passage across the blood–brain barrier (BBB) with its tight intercellular junctions, molecular components and transporter systems. Consequently, it is critical to identify the extent of brain permeation and the partitioning across the BBB. The interpretation of brain‐to‐blood ratios is considered to be a significant and fundamental approach for estimating drug penetration through BBB, the brain‐targeting ability and central nervous system (CNS) pharmacokinetics. Among the different bioanalytical techniques, liquid chromatography with various detectors has been widely used for determination of these ratios. This review defines the different approaches for sample preparation, extraction techniques and liquid chromatography procedures concerned with the determination of drugs in blood and brain tissues and the assessment of brain‐to‐blood levels. These approaches are expanded to cover the analysis of several drug classes such as CNS‐acting drugs, chemotherapeutics, antidiabetics, herbal medicinal products, radiopharmaceuticals, antibiotics and antivirals. Accordingly, stability in biological matrices and matrix effects are investigated. The different administration/formulation effects and the possible deviations in these ratios are also disscussed.

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