Mechanism of brain targeting by dexibuprofen prodrugs modified with ethanolamine-related structures.

ABSTRACT: The first molecular insights into how prodrugs modified with ethanolamine-related structures target the brain were generated using an in vitro BBB model and in situ perfusion technique. Prodrugs were delivered safely and efficiently to the brain through tight interaction with the anionic membrane of brain capillary endothelial cells, observed as a shift in zeta potential, followed by uptake into the cells. Prodrugs III and IV carrying primary and secondary amine modifications appeared to enter the brain via energy-independent passive diffusion. In contrast, besides the passive diffusion, prodrugs I and II carrying tertiary amine modifications also appeared to enter via an active process that was energy and pH dependent but was independent of sodium or membrane potential. This active proces

SUBMITTER: Li Y 

PROVIDER: S-EPMC4671119 | biostudies-literature | 2015 Dec

REPOSITORIES: biostudies-literature