INNOVATIVE FUNCTIONAL SYSTEMS FOR DELIVERY OF AMINOQUINOLINES AND DERIVATIVES THEREOF BASED ON DENTRITIC POLYMERS WITH MITOCHONDRIA TARGETING CAPACITY

摘要

The present invention relates to the development of innovative functional systems for drug delivery based on dendritic polymers which have on their surface suitable groups which make them capable to target cell mitochondria, in particular cancer cell mitochondria. These systems enclose bioactive molecules belonging to the class of aminoquinolines and derivatives thereof, which have a small therapeutic effect on cancers or any therapeutic effect of which is achieved at doses higher than the tolerable/allowable one. These compounds may be enclosed in the above systems either alone or in combination with known cytostatics e.g. compounds from the class of anthracyclines. These systems have been modified with functional groups so that they pass through both a cellular membrane and a mitochondrial membrane and thus the enclosed drugs are delivered and released therein. In this way, a 10- to 100-times enhanced cytotoxicity against cancer cell lines, compared to that of the respective non-enclosed drugs, is induced.