Using 5-fluorouracil-encored plga nanoparticles for the treatment of colorectal cancer: the in-vitro characterization and cytotoxicity studies

Colorectal cancer (CRC) is a prevalent cancer worldwide. The present study aimed to synthesize and investigate the potential of wheat germ agglutinin (WGA) conjugated with polylactic-co-glycolic acid (PLGA) nanoparticles (NPs) incorporating 5-fluorouracil (5-FU).

The NPs were investigated in terms of various characteristics, such as the particle size, surface charge, surface morphology, entrapment efficiency rate, and in-vitro drug release profile in simulated gastric and intestinal fluids. The optimized NPs were conjugated with WGA and characterized for the WGA conjugation efficiency, mucoadhesion, and cytotoxicity studies.

The zeta potential of the WGA-conjugated NPs decreased (-17.9±1.4 mV) possibly due to the conjugation of the NPs with WGA, which reduced the zeta potential. The WGA-conjugated NPs exhibited sustained drug release effects (p<0.05) compared to the marketed formulation containing 5-FU after 24 hours. In addition, the optimized NPs followed the Higuchi kinetics, showing diffusion-controlled drug release mechanisms. Finally, the WGA-conjugated PLGA NPs could significantly inhibit the growth of colon cancer cells (HT-29 and COLO-205) compared to the non-conjugated NPs and pure drug solution (P<0.05).

According to the results, the WGA-conjugated NPs could be potential carrier systems compared to the non-conjugated NPs for the effective management of CRC.