5-Fluorouracil-loaded polylactic acid nanoparticles have a killing effect on gastric cancer cell lines in vitro

Li Xiao-li; Niu Min; Zhang Ming; Zhang Na-na; Shi Yao

doi:10.3969/j.issn.2095-4344.2015.38.020

Abstract：BACKGROUND:5-Fluorouracil occupies an important position in the treatment of gastric cancer, but its long-term use can easily induce adverse reactions such as myelosuppression and leukopenia. Polylactic acid and its copolymers have a higher biocompatibility, and their decomposer cannot gather in the body. <br> OBJECTIVE:To investigate the in vitro cytotoxicity mechanism of 5-fluorouracil-loaded polylactic acid nanoparticles on gastric cancer cel lines. <br> METHODS:Ten mice were selected in this study. 5-fluorouracil-loaded polylactic acid nanoparticles (1×10-7, 1×10-6, 1×10-5, 1×10-4 mol/L) were prepared using ultrasonic emulsification method. Kiling effect of polylactic acid nanoparticles on gastric cancer cel lines in vitrowere detected. Then, the inhibition rate was calculated at different concentrations. <br> RESULTS AND CONCLUSIONS: Under the transmission electron microscope, 5-fluorouracil-loaded polylactic acid nanoparticles had good shape and relatively evenly distributed with no adhesions. After drug administration, the drug concentration was 50% at 24 hours and 62.9% at 72 hours. After 48 hours co-culture with single 5-fluorouracil or 5-fluorouracil-loaded polylactic acid nanoparticles, the viability of gastric cancer cels showed a decrease trend with the increase of drug concentrations, and moreover, 5-fluorouracil-loaded polylactic acid nanoparticles had a better cel inhibition ability than the single 5-fluorouracil (P < 0.05). The IC50value of 5-fluorouracil-loaded polylactic acid nanoparticles was significantly lower than that of 5-fluorouracil (P < 0.05). These findings indicate that polylactic acid nanoparticles as good drug carriers have a strong drug loading capacity and increase drug concentration in the body, but cannot reduce the biological activity of 5-fluorouracil, which provide new ideas for the treatment of gastric cancer.