Cetuximab scFv-modified 5-FU Loaded Chitosan Nanoparticles: A Novel Therapeutic Platform.

BACKGROUND

Colorectal cancer (CRC) is among the most fatal types of cancer. An active targeting delivery system that specifically interacts with CRC cells could improve the therapy's outcomes. Herein, Cetuximab single-chain fragment variable antibody (scFv) fragments were conjugated to the surface of 5-FU encapsulated chitosan nanoparticles (CS NPs) to develop an effective therapeutic platform (scFv-CS/5-FU NPs).

METHODS

CS/5-FU NPs were synthesized using a special fluidic system. Encapsulation efficiency (EE), loading capacity (LC), and the drug release profile of the particles were determined. scFv fragments were produced recombinantly and tailored on the surface of CS/5-FU NPs. The physicochemical features of scFv-CS/5-FU NPs were also characterized. MTT and flow cytometry assay investigated the toxicity effect of scFv-CS/5-FU NPs on the HCT116 cell line.

RESULTS

CS/5-FU NPs had a homogenous spherical shape. They possessed sustainable drugrelease behavior. The produced scFv-CS/5-FU NPs were also spherical. scFv-CS/5-FU NPs significantly decreased the viability of cancerous cells in a dose-dependent manner and induced apoptosis in 97.97% of targeted cells.

CONCLUSION

scFv-CS/5-FU NPs showed remarkable anti-CRC activity. This novel targeting delivery system reduced the effective dose of 5-FU which is of vital importance to decrease the devastating side effects of chemotherapy.