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 |
|---|---|
| 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 |
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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
Cite this
Recent advances in the brain targeting of neuropharmaceuticals by chemical delivery systems. / Bodor, Nicholas; Buchwald, Peter.
In: Advanced Drug Delivery Reviews, Vol. 36, No. 2-3, 05.04.1999, p. 229-254.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Recent advances in the brain targeting of neuropharmaceuticals by chemical delivery systems
AU - Bodor, Nicholas
AU - Buchwald, Peter
PY - 1999/4/5
Y1 - 1999/4/5
N2 - 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.
AB - 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.
KW - Blood-brain barrier
KW - Brain-targeted redox analog
KW - Cyclodextrin
KW - Estradiol
KW - Neuropeptides
KW - Octanol-water partition
KW - P-glycoprotein
KW - Retrometabolic design
KW - Zidovudine (AZT)
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UR - http://www.scopus.com/inward/citedby.url?scp=0033526158&partnerID=8YFLogxK
U2 - 10.1016/S0169-409X(98)00090-8
DO - 10.1016/S0169-409X(98)00090-8
M3 - Article
AN - SCOPUS:0033526158
VL - 36
SP - 229
EP - 254
JO - Advanced Drug Delivery Reviews
JF - Advanced Drug Delivery Reviews
SN - 0169-409X
IS - 2-3
ER -