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Folic acid tagged Chitosan nanoparticle loaded with novel drug “copper acetylacetonate” for efficient cancer cell targeting. Arindam Pramanik & Parimal Karmakar* Department of Life Science and Biotechnology, Jadavpur University, Kolkata 700032, India *Corresponding author E-mail: [email protected] Objective: To develop a biodegradable & non-toxic nanoparticle for cancer cell delivery. To choose an efficient anticancer drug. To make hydrophobic modification in the nanoparticle for proper loading of the anticancer drug. To specifically target the nanoparticle to cancer cells for minimizing any toxic effect on healthy cells. Result: In this work we have developed a novel non-toxic, biodegradable chitosan nanoparticle which is hydrophobically modified at its core for various hydrophobic drug encapsulations. Folic acid is conjugated on the surface of the nanoparticle for targeting of cancer cells. We have also explored the synergistic anti-cancer activity of copper ion and acetylacetone complex containing 1,3 diketone group (like curcumin) in Copper acetylacetonate (CuAA). The cytotoxicity of the CuAA complex was evaluated on various cancer cells. Among the mechanisms, reactive oxygen species (ROS), glutathione level (GSH) in the cell was found to increase upon treatment with CuAA along with mitochondrial membrane damage. Further this reagent induced apoptosis mediated cell death. For application of this novel drug as a therapeutic and to overcome the problem of solubility of CuAA, it is loaded into the folic acid tagged hydrophobic chitosan nanoparticle. Conclusion: This novel CuAA has an efficient anticancer activity. For its specific targeting of cancer cells and minimizing toxicity to healthy cells the hydrophobic chitosan nanoparticle tagged with folic acid is an excellent strategy. Thus CuAA encapsulated in the chitosan nanoparticle can be a potential anticancer therapeutic agent.