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 language | English |
|---|---|
| Pages (from-to) | 161-175 |
| Number of pages | 15 |
| Journal | American Journal of Drug Delivery |
| Volume | 4 |
| Issue number | 3 |
| DOIs | |
| State | Published - Sep 12 2006 |
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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 journal › Article
}
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
AN - SCOPUS:33748374488
VL - 4
SP - 161
EP - 175
JO - American Journal of Drug Delivery
JF - American Journal of Drug Delivery
SN - 1175-9038
IS - 3
ER -