Drug Penetration into the Central Nervous System: Pharmacokinetic Concepts and In Vitro Model Systems.

ABSTRACT: Delivery of most drugs into the central nervous system (CNS) is restricted by the blood-brain barrier (BBB), which remains a significant bottleneck for development of novel CNS-targeted therapeutics or molecular tracers for neuroimaging. Consistent failure to reliably predict drug efficiency based on single measures for the rate or extent of brain penetration has led to the emergence of a more holistic framework that integrates data from various in vivo, in situ and in vitro assays to obtain a comprehensive description of drug delivery to and distribution within the brain. Coupled with ongoing development of suitable in vitro BBB models, this integrated approach promises to reduce the incidence of costly late-stage failures in CNS drug development, and could help to overcome some of the te

SUBMITTER: Neumaier F 

PROVIDER: S-EPMC8538549 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature