Development and Evaluation of Crocetin-Functionalized Pegylated Magnetite Nanoparticles for Hepatocellular Carcinoma

Liver cancer remains among the leading causes of cancer-related deaths worldwide. This is due to many reasons, including limitations of available drugs, late diagnosis due to the overlapping symptoms with many other liver diseases, and lack of effective screening modalities. Compared to conventional chemotherapy, targeted drug delivery systems are advantageous in many ways, as they minimize drug resistance and improve therapeutic value for cancer patients. Nanomaterials, in general, and nanoparticles, in particular, possess nm size, which provides a high surface area for a great extent of functionalization to be used for the targeted delivery of cancer drugs. Amongst the different formulations of nanoparticles, magnetic nanoparticles (MNPs) have unique chemical and physical characteristics and magnetic behavior, making them preferable candidates as a core for drug delivery systems. To maintain the nanosized structure of MNPs, a polymeric coating is usually applied to maintain the nanoparticles dispersed in the solution. Moreover, the polymeric coating provides a plate form for carrying drug molecules on its surface. In the present study, poly(ethylene glycol) (PEG)-coated MNPs were successfully synthesized, where the optimum concentration of PEG on the surface of the MNPs was investigated. The PEG-coated MNPs were further coated with crocetin at different concentrations. The crocetin-coated pegylated MNPs were evaluated in vitro using a hepatic cell line (HepG2) for up to 72 h. Results showed good release kinetics under acidic and neutral conditions. The optimally prepared drug delivery system showed a high potential for reducing the HepG2 cell proliferation in vitro using an MTT assay. The calculated IC50 for Cro-PEG-MNPs were 0.1019, 0.0903, and 0.0462 mg/mL of 5x, 10x and 20x, respectively.

Automated summary

Liver cancer remains a major cause of cancer-related deaths, partly due to limitations of available drugs and late diagnosis. Targeted drug delivery systems using nanoparticles, especially magnetic nanoparticles (MNPs), show promise in improving therapeutic value by reducing drug resistance. In this study, PEG-coated MNPs were successfully synthesized and coated with crocetin at different concentrations. The crocetin-coated pegylated MNPs demonstrated good release kinetics under acidic and neutral conditions and showed potential in reducing the proliferation of HepG2 cells in vitro.