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Adv Drug Deliv Rev. 1999 Apr 5;36(2-3):229-254.

Recent advances in the brain targeting of neuropharmaceuticals by chemical delivery systems.

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Center for Drug Discovery, University of Florida, Health Science Center, PO Box 100497, Gainesville, FL 32610-0497, USA


Brain-targeted chemical delivery systems represent a general and systematic method that can provide localized and sustained release for a variety of therapeutic agents including neuropeptides. By using a sequential metabolism approach, they exploit the specific trafficking properties of the blood-brain barrier and provide site-specific or site-enhanced delivery. After a brief description of the design principles, the present article reviews a number of specific delivery examples (zidovudine, ganciclovir, lomustine benzylpenicillin, estradiol, enkephalin, TRH, kyotorphin), together with representative synthetic routes, physicochemical properties, metabolic pathways, and pharmacological data. A reevaluated correlation for more than 60 drugs between previously published in vivo cerebrovascular permeability data and octanol/water partition coefficients is also included since it may be useful in characterizing the properties of the blood-brain barrier, including active transport by P-glycoprotein.


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