Molecular theranostic based on esterase-mediated drug activation for hepatocellular carcinoma

Abstract

In past few years, cancer specific targeted drug formulations have shown some hope of improving the therapeutics with minimized associated side effects of chemotherapy. However, the benefits has proven modest due to lack of systems that can be assessed easily from parent drugs while maintaining the same features of cancer associated prodrug activation. We developed a small molecule-based, carboxylesterase responsive theranostic, EDOX, with tumor-specific enzymatic activation for targeted delivery of the anticancer drug, Doxorubicin (Dox), to hepatocellular carcinoma (HCC) cells. Easy synthetic access, physiological stability, tumor-selective activation, and sustained drug release make EDOX an excellent candidate for use as a next-generation drug delivery system for HCC.