IN-VIVO ELIMINATION OF DIHYDROPYRIDINE DRUG DELIVERY CARRIERS FROM BRAIN AND BLOOD OF RATS

Document Type : Original Article

Authors

1 Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, U.S.A

2 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt

Abstract

The dihydropyridine « pyridinium salt redox delivery system, used for specific delivery and sustained release of drugs in the brain was studied. The rates of elimination of the ester and acid metabolites of l-methyl- 3-(ethoxycarbonyl)-1,4-dihydrpyridine and of 1-(2-ethoxycarbonyl) ethyl-1,4-dihydronicotinamide from brain and blood of rats after systemic administration of dihydro carrier-ethanol couples were investigated, taking ethanol as a model drug. It was found that the quaternary species are eliminated relatively fast, which supports the hypothesis for existence of an active transport mechanism for eliminating organic ions from the brain. The results can serve as a primary evidence for the suggestion that the carrier and its metabolites will not impair central nervous system functions.