Curcumin Surfactant as Anticancer Prodrugs and Drug Carriers

Hydrophobic curcumin is conjugated to short PEG chains to form an amphiphilic surfactant structure. This surfactant forms stable nanoparticles in aqueous conditions and thus serves two roles: It is water-soluble and stable and has comparable cytotoxicity to curcumin to cancer cells, and thus can be used as an anticancer prodrug. The formed nanoparticle can be used as carriers for other anticancer drugs such as doxorubicin (DOX) and camptothecin (CPT) to synergize their anticancer efficacies. As an anticancer prodrug, the surfactant shows significant in vitro cytotoxicities to human ovarian cancer (SKOV-3, OVCAR), breast cancer (MCF-7) and colon cancer cell lines with an IC50 of 4.4, 1.8, 7.7, 1.9 ėg/mL curcumin-equivalent dose, respectively. The surfactant arrests SKOV cell cycle at the G0/G1 phase and induces cell apoptosis through caspase-3-dependent pathway. In vivo, the surfactant demonstrates remarkable antitumor and tumor prevention activities in xenograft mice model. As a drug carrier, the surfactant has a critical micelle concentration of about 50 ėg/mL and can be loaded with DOX and CPT inside the micelles with a loading efficiency of 36% and 57%, respectively.