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Sci Rep. 2013 Oct 4;3:2859. doi: 10.1038/srep02859.

Molecular imaging of drug transit through the blood-brain barrier with MALDI mass spectrometry imaging.

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1
Department of Neurosurgery, Brigham and Women's Hospital, Harvard Medical School, Boston MA.

Abstract

Drug transit through the blood-brain barrier (BBB) is essential for therapeutic responses in malignant glioma. Conventional methods for assessment of BBB penetrance require synthesis of isotopically labeled drug derivatives. Here, we report a new methodology using matrix assisted laser desorption ionization mass spectrometry imaging (MALDI MSI) to visualize drug penetration in brain tissue without molecular labeling. In studies summarized here, we first validate heme as a simple and robust MALDI MSI marker for the lumen of blood vessels in the brain. We go on to provide three examples of how MALDI MSI can provide chemical and biological insights into BBB penetrance and metabolism of small molecule signal transduction inhibitors in the brain - insights that would be difficult or impossible to extract by use of radiolabeled compounds.

PMID:
24091529
PMCID:
PMC3790202
DOI:
10.1038/srep02859
[Indexed for MEDLINE]
Free PMC Article
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