Redox systems for brain-targeted drug delivery
AssigneeUniversity of Florida
InventorNicholas S. Bodor
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Abstract
Inclusion complexes of hydroxypropyl, hydroxyethyl, glucosyl, maltosyl and maltotriosyl derivatives of .beta.- and .gamma.-cyclodextrin with the reduced, biooxidizable, blood-brain barrier penetrating, lipoidal forms of dihydropyridine.revreaction.pyridinium salt redox systems for brain-targeted drug delivery provide a means for stabilizing the redox systems, particularly against oxidation. The redox inclusion complexes also provide a means for decreasing initial drug concentrations in the lungs after administration of the systems, leading to decreased toxicity. In selected instances, complexation results in substantially improved water solubility of the redox systems as well.
Claims72
A method for stabilizing the reduced, biooxidizable, blood-brain barrier penetrating, lipoidal dihydropyridine form of a dihydropyridine .revreaction. pyridinium salt redox system for brain-targeted drug delivery, said method comprising complexing said dihydropyridine form with cyclodextrin selected from the group consisting of hydroxyethyl, glucosyl, maltosyl and maltotriosyl derivatives of .beta.-cyclodextrin and hydroxypropyl, hydroxyethyl, glucosyl, maltosyl and maltotriosyl derivatives of .tau.-cyclodextrin.
A method for decreasing initial lung concentrations of drug resulting from administration of the reduced, booxidizable, blood-brain barrier penetrating, lipoidal dihydropyridine form of a dihydropyridine .revreaction. pyridinium salt redox system for brain-targeted drug delivery, said method comprising administering said dihydropyridine form as its inclusion complex with cyclodextrin selected from the group consisting of hydroxyethyl, glucosyl, maltosyl and maltotriosyl derivatives of .beta.-cyclodextrin and hydroxypropyl, hydroxyethyl, glucosyl, maltosyl and maltotriosyl derivatives of .tau.-cyclodextrin.
A method for decreasing the tendency of the reduced, biooxidizable, blood-brain barrier penetrating, lipoidal dihydropyridine form of a dihydropyridine .revreaction. pyridinium salt redox system for brain-targeted drug delivery to provide high initial concentrations of drug in the lungs following administration, said method comprising complexing said dihydropyridine form with cyclodextrin selected from the group consisting of hydroxyethyl, glucosyl, maltosyl and maltotriosyl derivatives of .beta.-cyclodextrin and hydroxypropyl, hydroxyethyl, glucosyl, maltosyl and maltotriosyl derivatives of .tau.-cyclodextrin prior to administration.
Dependencies are inferred from the claim text.