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A novel chemical delivery system for brain targeting.

Two different chemical approaches for brain drug delivery and targeting are
proposed in the present review.

One is a chemical drug delivery using a ring-closure reaction to the
hydrophilic quaternary thiazolium compound in the brain.

The other is a chemical drug targeting utilizing the nutrient receptor
(transporter) system on the blood-brain barrier.

The brain delivery system has been optimized and it was demonstrated that
the brain delivery of three drugs,
- a drug for Parkinson's disease,
- an excitatory amino acid antagonist and
- a free radical scavenger,
were improved by the conjugation with cis-2-formylaminoethenylthio
derivatives in vivo.

As for the brain targeting system, it was demonstrated that the conjugation
with L-Glu improved the drug's brain distribution via the L-Glu excitatory
and/or transport receptors in vitro and in vivo.

These findings suggest that the concepts of two chemical approaches will
contribute to the development of new central nervous system drugs.


Adv Drug Deliv Rev 1999 Apr 5;36(2-3):255-275
Yoshikawa T, Sakaeda (nee Kakutani) T, Sugawara T, Hirano K, Stella VJ
Shionogi Research Laboratories, Shionogi & Co. Ltd., Osaka 553-0002, Japan
PMID: 10837719

http://www.ncbi.nlm.nih.gov:80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list
_uids=10837719&dopt=Abstract


janet paterson
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