Experimental Insights and Recommendations for Successfully Performing Cerebral Microdialysis With Hydrophobic Drug Candidates.

ABSTRACT: Cerebral microdialysis in rodents represents a robust and versatile technique for quantifying the pharmacologically relevant unbound fraction of drugs in the brain. When this unbound fraction is simultaneously determined in plasma, it facilitates the calculation of the corresponding unbound plasma-to-brain partition coefficient (K_p,uu) for a given compound in vivo. This coefficient is critical for understanding the penetration and distribution of drugs across the blood-brain barrier (BBB). However, obtaining valid and accurate microdialysis data can be particularly challenging for hydrophobic drugs due to their pronounced non-specific interactions with the components of the microdialysis system. The present study reports the outcomes of comprehensive microdialysis investigations

SUBMITTER: Sundheimer JK 

PROVIDER: S-EPMC12033007 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature