ARGININE- AND ACRYLONITRILE-MODIFIED CHITOSAN NANOPARTICLES FOR ANTICANCER DRUG DELIVERY

Chitosan (CS) is an excellent natural biodegradable and biocompatible polymer for biomedical applications, however, its poor solubility in water or organic solvents limits its applications in drug delivery. In order to resolve this problem, chitosan was modified with acrylonitrile (AN) and arginine (Arg), the modified chitosan (AN–CS–Arg) was characterized by 1H NMR and Fourier transform infrared (FTIR). The AN–CS–Arg was self-assembled into nanoparticles to encapsulate anticancer drug doxorubicin (DOX). The size and morphology of the blank and drug-loaded AN–CS–Arg (AN–CS–Arg/DOX) nanoparticles were measured by dynamic light scattering (DLS), scanning electron microscopy (SEM) and atomic force microscopy (AFM). The mean size of both blank and AN–CS–Arg/DOX nanoparticles were around 50 nm and 170 nm, respectively. The drug-loading content was about 12%. The release profile of AN–CS–Arg/DOX nanoparticles was investigated in vitro, 80% encapsulated DOX could be released within 80 h. The AN–CS–Arg nanoparticles were nontoxic to both NIH 3T3 fibroblasts and HepG2 cancer cells. The cellular uptake of the AN–CS–Arg nanoparticles was trafficked via Confocal Laser Scanning Microscopy and Flow Cytometry, both results showed that the AN–CS–Arg nanoparticles could be internalized in HepG2 cells efficiently. The IC50 of AN–CS–Arg/DOX nanoparticles to HepG2 cancer cells was 10.0 μg/mL. The AN–CS–Arg nanoparticles are potential carriers for anticancer drug delivery.