Background: Scientists have extensively investigated curcumin, yielding many publications
on treatments of cancer. Numerous derivatives of curcumin were synthesized, evaluated for
their anti-oxidant and free-radical scavenging, SAR, ADME properties and tested in anticancer applications.
Objective: We decided to exploit curcumin as a bioactive core platform for carrying anticancer
drugs, which likely possesses a carboxyl moiety for potential linkage to the carrier for drug delivery.
Methods: The goal of this work is to develop biolabile multifunctional curcumin platforms towards
anticancer drug delivery, including determination of drug release profiling in hydrolytic
media, in vitro cytotoxicity, antioxidant properties and blockage of relevant cell survival pathways.
Results: We report on a facile synthesis of the bioactive multifunctional curcumin-based platforms
linked to a variety of anticancer drugs like amonafide and chlorambucil, and release of the drugs in
a hydrolytic environment. The leading curcumin-based platform has presented antioxidant activity
similar to curcumin, but with much more potent cytotoxicity in vitro in agreement with the augmented
blockage of the NF-kB cell survival pathway.
Conclusion: The approach presented here may prove beneficial for bioactive curcumin-based delivery
applications where multiple drug delivery is required in a consecutive and controlled mode.