"All in the mind"? Brain-targeting chemical delivery system of 17β-estradiol (Estredox) produces significant uterotrophic side effect.

ABSTRACT: Here we revisit the peculiarly named redox chemical delivery system concept. This unique prodrug approach has long been claimed to be capable of targeting 17β-estradiol (E2), which has numerous beneficial central effects, into the brain without detrimental peripheral hormonal exposure. Using a well-established protocol to monitor E2's antidepressant-like effect, we show that the administration of this chemical delivery system incorporated into hydroxypropyl-β-cyclodextrin (i.e., Estredox), indeed, triggers a transient antidepressant-like behavior in ovariectomized mice. At the same time, even an acute dose of the carefully purified chemical delivery system produces significant circulating E2 levels and uterotrophic side effects for several days after drug administration. For the first time

SUBMITTER: Prokai-Tatrai K 

PROVIDER: S-EPMC3874273 | biostudies-literature | 2012

REPOSITORIES: biostudies-literature