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. Copyright (C) 1999 Elsevier Science B.V.
Original language | English (US) |
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Pages (from-to) | 229-254 |
Number of pages | 26 |
Journal | Advanced Drug Delivery Reviews |
Volume | 36 |
Issue number | 2-3 |
DOIs | |
State | Published - Apr 5 1999 |
Externally published | Yes |
Keywords
- Blood-brain barrier
- Brain-targeted redox analog
- Cyclodextrin
- Estradiol
- Neuropeptides
- Octanol-water partition
- P-glycoprotein
- Retrometabolic design
- Zidovudine (AZT)
ASJC Scopus subject areas
- Pharmaceutical Science