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Updated: Aug 10, 2026

Systemic and Local Drug Delivery for Treating Diseases of the Central Nervous System in Rodent Models
Published on: August 16, 2010
Recent advances in the brain targeting of neuropharmaceuticals by chemical delivery systems
1Center for Drug Discovery, University of Florida, Health Science Center, PO Box 100497, Gainesville, FL 32610-0497, USA
Abstract:
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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