BRAIN-SPECIFIC DRUG DELIVERY

摘要

The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are: (a) compounds of the formula: ¨ADD-DHC¨BD (I), wherein ¨ADD¨BD is a centrally acting drug species, and ¨ADDHC¨BD is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine$(1,10)$pyridinium salt redox carrier, with the proviso that when ¨ADDHC¨BD is$(10,)$wherein R is lower alkyl or benzyl and ¨ADD¨BD is a drug species containing a single NH2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH2 or OH functional group to the carbonyl function of ¨ADDHC¨BD, then ¨ADD¨BD must be other than a sympathetic stimulant, steroid sex hormone, memory enhancer, long chain alkanol or anticancer or antitumor agent; and (b) non-toxic pharmaceutically acceptable salts of compounds of formula (I) wherein ¨ADD¨BD is a centrally acting drug species and ¨ADDHC¨BD is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine$(1,10)$pyridinium salt redox carrier. The correspnding ionic pyridinium salt type drug/carrier entities ¨ADD-QC¨BD+ are also disclosed, as are derivatives of testicularly acting drug species capable of penetrating the blood-testis barrier.