Brain-targeted delivery of estradiol

Therapeutic potential and results obtained with a chemical delivery system approach

Nicholas Bodor, Peter Buchwald

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Estradiol is the most potent human estrogen, and because many of its pharmacologic effects are mediated through the central nervous system (CNS), there are several potential therapeutic applications for a system that could achieve brain-targeted delivery. By directing the active compound away from the circulatory system and behind the blood-brain barrier, brain-targeting should increase treatment efficiency for CNS-mediated effects and reduce the likelihood of peripheral adverse effects, such as increased risks for cancer (the main reason many women avoid traditional hormone therapy). Possible therapeutic applications include the treatment of menopausal vasomotor symptoms (hot flashes), the treatment and/or prevention of various types of dementia (including Alzheimer disease), treatment of male or female sexual dysfunction, and possibly neuroprotection. Preclinical and clinical results obtained with an estradiol chemical delivery system, an innovative chemical entity that uses a redox CDS approach to selectively target estradiol to the brain and CNS by releasing it following a designed metabolic sequence, demonstrate effective brain-targeting and long-lasting pharmacologic activity, thus confirming the potential of this approach.

Original languageEnglish
Pages (from-to)161-175
Number of pages15
JournalAmerican Journal of Drug Delivery
Volume4
Issue number3
DOIs
StatePublished - Sep 12 2006
Externally publishedYes

Fingerprint

Estradiol
Brain
Central Nervous System
Therapeutics
Hot Flashes
Cardiovascular System
Blood-Brain Barrier
Oxidation-Reduction
Dementia
Alzheimer Disease
Estrogens
Hormones
Neoplasms

ASJC Scopus subject areas

  • Pharmacology

Cite this

Brain-targeted delivery of estradiol : Therapeutic potential and results obtained with a chemical delivery system approach. / Bodor, Nicholas; Buchwald, Peter.

In: American Journal of Drug Delivery, Vol. 4, No. 3, 12.09.2006, p. 161-175.

Research output: Contribution to journalArticle

@article{85e8b16b473947f3a6860713e98ee144,
title = "Brain-targeted delivery of estradiol: Therapeutic potential and results obtained with a chemical delivery system approach",
abstract = "Estradiol is the most potent human estrogen, and because many of its pharmacologic effects are mediated through the central nervous system (CNS), there are several potential therapeutic applications for a system that could achieve brain-targeted delivery. By directing the active compound away from the circulatory system and behind the blood-brain barrier, brain-targeting should increase treatment efficiency for CNS-mediated effects and reduce the likelihood of peripheral adverse effects, such as increased risks for cancer (the main reason many women avoid traditional hormone therapy). Possible therapeutic applications include the treatment of menopausal vasomotor symptoms (hot flashes), the treatment and/or prevention of various types of dementia (including Alzheimer disease), treatment of male or female sexual dysfunction, and possibly neuroprotection. Preclinical and clinical results obtained with an estradiol chemical delivery system, an innovative chemical entity that uses a redox CDS approach to selectively target estradiol to the brain and CNS by releasing it following a designed metabolic sequence, demonstrate effective brain-targeting and long-lasting pharmacologic activity, thus confirming the potential of this approach.",
author = "Nicholas Bodor and Peter Buchwald",
year = "2006",
month = "9",
day = "12",
doi = "10.2165/00137696-200604030-00004",
language = "English",
volume = "4",
pages = "161--175",
journal = "American Journal of Drug Delivery",
issn = "1175-9038",
publisher = "Adis International Ltd",
number = "3",

}

TY - JOUR

T1 - Brain-targeted delivery of estradiol

T2 - Therapeutic potential and results obtained with a chemical delivery system approach

AU - Bodor, Nicholas

AU - Buchwald, Peter

PY - 2006/9/12

Y1 - 2006/9/12

N2 - Estradiol is the most potent human estrogen, and because many of its pharmacologic effects are mediated through the central nervous system (CNS), there are several potential therapeutic applications for a system that could achieve brain-targeted delivery. By directing the active compound away from the circulatory system and behind the blood-brain barrier, brain-targeting should increase treatment efficiency for CNS-mediated effects and reduce the likelihood of peripheral adverse effects, such as increased risks for cancer (the main reason many women avoid traditional hormone therapy). Possible therapeutic applications include the treatment of menopausal vasomotor symptoms (hot flashes), the treatment and/or prevention of various types of dementia (including Alzheimer disease), treatment of male or female sexual dysfunction, and possibly neuroprotection. Preclinical and clinical results obtained with an estradiol chemical delivery system, an innovative chemical entity that uses a redox CDS approach to selectively target estradiol to the brain and CNS by releasing it following a designed metabolic sequence, demonstrate effective brain-targeting and long-lasting pharmacologic activity, thus confirming the potential of this approach.

AB - Estradiol is the most potent human estrogen, and because many of its pharmacologic effects are mediated through the central nervous system (CNS), there are several potential therapeutic applications for a system that could achieve brain-targeted delivery. By directing the active compound away from the circulatory system and behind the blood-brain barrier, brain-targeting should increase treatment efficiency for CNS-mediated effects and reduce the likelihood of peripheral adverse effects, such as increased risks for cancer (the main reason many women avoid traditional hormone therapy). Possible therapeutic applications include the treatment of menopausal vasomotor symptoms (hot flashes), the treatment and/or prevention of various types of dementia (including Alzheimer disease), treatment of male or female sexual dysfunction, and possibly neuroprotection. Preclinical and clinical results obtained with an estradiol chemical delivery system, an innovative chemical entity that uses a redox CDS approach to selectively target estradiol to the brain and CNS by releasing it following a designed metabolic sequence, demonstrate effective brain-targeting and long-lasting pharmacologic activity, thus confirming the potential of this approach.

UR - http://www.scopus.com/inward/record.url?scp=33748374488&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33748374488&partnerID=8YFLogxK

U2 - 10.2165/00137696-200604030-00004

DO - 10.2165/00137696-200604030-00004

M3 - Article

VL - 4

SP - 161

EP - 175

JO - American Journal of Drug Delivery

JF - American Journal of Drug Delivery

SN - 1175-9038

IS - 3

ER -