Evaluation of an estradiol chemical delivery system (CDS) designed to provide enhanced and sustained hormone levels in the brain
作者： K.S. Estes , M.E. Brewster , N. Bodor
DOI: 10.1016/0169-409X(94)90037-X
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摘要: Abstract While estrogens readily penetrate the blood-brain barrier and exert significant CNS effects, they are not retained by this organ, obligating constant dosing to achieve sustained pharmacologically relevant brain concentrations. Such a regimen also generates high peripheral levels of which have been linked metabolic disturbance cancer. Brain-selective targeting would act increase safety administered drugs sparing non-target-site tissues. A dihydronicotinate-nicotinate redox targetor designed along these lines was found be successful in maintaining central estradiol while were rapidly eliminated. In human clinical trials, estradiol-chemical delivery system (E2-CDS) reduced circulating LH greater extent than did but caused less an blood levels.
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