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

Nicholas Bodor, Peter Buchwald

Research output: Contribution to journalReview articlepeer-review

155 Scopus citations


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 languageEnglish (US)
Pages (from-to)229-254
Number of pages26
JournalAdvanced Drug Delivery Reviews
Issue number2-3
StatePublished - Apr 5 1999
Externally publishedYes


  • 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


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