PMID: 16526562Mar 11, 2006Paper

Comparative evaluation of Estredox, a brain-targeted estradiol delivery system versus traditional estrogen replacement therapy

Die Pharmazie
I SzirákiN Bodor

Abstract

Estredox is a novel brain-targeted delivery system for estradiol (E2). The mechanism of this estradiol-chemical delivery system (E2-CDS) is based on an interconvertible dihydropiridine <--> pyridinium salt carrier (targetor) attached to E2. After administration of the E2-CDS, the targetor moiety is oxidized to a quaternary pyridinium salt (E2-Q+). Here we demonstrate that a single i.v. injection with E2-CDS (3 mg/kg) resulted in sustained presence of E2-Q+ in three various brain regions. The sustained and gradual release of estradiol from E2-Q+ is reflected by the time-course of plasma estrogen level. At the end of repeated administration of E2-CDS (daily once 0.3 mg/kg i.v. for 10 consecutive days) we found a sharp decrease in the levels of plasma estradiol followed by a gradual decrease. The levels of E2-Q+ in the investigated brain regions decreased gradually from the first post-treatment day, however, a detectable amount of E2-Q+ was still present in the hypothalamus, striatum, and cortex even on the 24th post-treatment day. Strikingly different plasma estradiol levels were found in the groups of orchidectomized rats that received daily i.v. injections of estradiol benzoate (E2-BZ). The plasma estradiol levels in these anim...Continue Reading

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