In vitro and in vivo evaluations of dihydroquinoline- and dihydroisoquinoline-based targetor moieties for brain-specific chemical delivery systems

Nicholas Bodor, Hassan H. Farag, M. Dulce C. Barros, Whei Mei Wu, Peter Buchwald

Research output: Contribution to journalArticlepeer-review

19 Scopus citations

Abstract

Brain-targeted delivery of various drugs can be successfully achieved by chemical delivery systems (CDS) that contain a 1,4-dihydropyridine-based redox targetor moiety and undergo a sequential metabolism. However, the susceptibility of this moiety toward hydration in acidic media may limit the shelf-life of such compounds in aqueous formulation. Here, a systematic investigation of the chemical stability toward oxidation and hydration of ester and amide derivatives of 3-substituted 1,4-dihydropyridine, 1,4-dihydroquinoline, and 4-substituted 1,2-dihydroisoquinoline is reported, together with the in vitro stability and in vivo (rat) distribution of isoquinoline-based testosterone and hydrocortisone chemical delivery systems, which were selected as having the most suitable acid-resistant targetor moieties.

Original languageEnglish (US)
Pages (from-to)63-71
Number of pages9
JournalJournal of Drug Targeting
Volume10
Issue number1
DOIs
StatePublished - 2002
Externally publishedYes

Keywords

  • Brain-targeted delivery
  • Dihydropyridine
  • Hydrocortisone
  • Redox
  • Testosterone

ASJC Scopus subject areas

  • Pharmaceutical Science

Fingerprint Dive into the research topics of 'In vitro and in vivo evaluations of dihydroquinoline- and dihydroisoquinoline-based targetor moieties for brain-specific chemical delivery systems'. Together they form a unique fingerprint.

Cite this