Site-specific, sustained release of drugs to the brain

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Science  18 Dec 1981:
Vol. 214, Issue 4527, pp. 1370-1372
DOI: 10.1126/science.7313698


A dihydropyridine-pyridinium salt type of redox system is used in a general and flexible method for the site-specific or sustained delivery (or both) of drugs to the brain. A biologically active compound linked to a lipoidal dihydropyridine carrier easily penetrates the blood-brain barrier. Oxidation of the carrier part in vivo to the ionic pyridinium salt prevents its elimination from the brain, while elimination from the general circulation is accelerated. Subsequent cleavage of the quaternary carrier-drug species results in sustained delivery of the drug in the brain and facile elimination of the carrier part.