Enhanced Targeting Function and Anti-colon Cancer Efficacy by Wheat Germ Agglutinin-modified Nanoparticles for Matrine Delivery

Background and Objective: A novel delivery system of matrine (MT) using Wheat Germ Agglutinin (WGA), an ideal bio-adhesive material, had been developed by us. The present work was aimed to evaluate the targeting function, anti-colon cancer efficacy and mechanisms of this novel delivery system on cell level. Materials and Methods: After WGA-modified matrine nanoparticles (WGA-MT-NPs) were prepared with our optimized methods, the Encapsulation Efficiency (EE) of MT and modification rate of WGA were measured by HPLC and folin-phenol method, respectively. Subsequently, Transmission Electron Microscopy (TEM) was used to further confirm the modification of WGA and HT-29 human colon cancer cells and NCM460 normal colonic epithelial cells were applied to assess the targeting function of WGA-MT-NPs. Furthermore, in HT-29 cells, the cell growth inhibition was determined by tetrazolium salt reagent (MTT) method and the apoptosis and cell cycle arrest were measured using flow cytometry assay. Results: The EE and modification rate of WGA were 89.99 +/- 5.08% and 87.57 +/- 8.61%, respectively. And, TEM revealed that WGA was effectively assembled on the surfaces of nanostructures. Moreover, WGA-MT-NPs possessed the specific affinity towards HT-29 cells, rather than NCM460 cells. In HT-29 cells, the growth inhibition rate was significantly improved by WGA-MT-NPs compared with MT-NPs. Furthermore, the apoptosis of HT-29 cells was significantly higher in WGA-MT-NPs than in MT-NPs. Conclusion: WGA-MT-NPs significantly increased the anti-tumor effect of MT-NPs via stronger affinity towards HT-29 cells and higher promotion of apoptosis. Thus, WGA-MT-NPs may provide a promising new strategy for anti-colon cancer.