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
N1 - Funding Information:
The contribution of the many collaborators mentioned in the references is gratefully acknowledged. Clinical trials have been supported by Pharmatec Inc. (Alachua, FL, USA), Pharmos Corporation (Iselin, NJ, USA) and IVAX Corporation (Miami, FL, USA).
PY - 2006
Y1 - 2006
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.
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U2 - 10.2165/00137696-200604030-00004
DO - 10.2165/00137696-200604030-00004
M3 - Review 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 -