RESUMO
OBJECTIVE: To investigate the anti-tumor activity of adriamycin-loaded chitosan nanoparticles surface-modified with glycyrrhizin on human hepatoma cell line SMMC-7721. METHODS: Inhibition effect of drug-loaded nanoparticle on the proliferation of SMMC-7721 cells was determined with MTT method. Intra-cellular distribution of nanoparticles and morphological change of SMMC-7721 cells before and after treatment were observed by confocal laser scanning microscope (CLSM) and the apoptosis induced by adriamycin was measured by TUNEL assay. RESULTS: The inhibition effect of adriamycin-loaded chitosan nanoparticles surface-modified with glycyrrhizin on the proliferation of SMMC-7721 cells increased 6.36 times lower in comparison with free drugs. The inhibition effect of adriamycin-loaded chitosan nanoparticles had no obvious improvement. Nanoparticles surface-modified with glycyrrhizin promoted the distrubition of adriamycin in the nucleus, so as to promote the anti-tumor activity of adriamycin. TUNEL assay indicated that nanoparticles surface-modified with glycyrrhizin induce DNA fragmentation and nucleus breakdown to induce the apoptosis of SMMC-7721 cells. CONCLUSION: Adriamycin-loaded chitosan nanoparticles surface-modified with glycyrrhizin can used as potential active hepatocyte-targeted delivery carrier. Pharmacokinetic evaluation of it is worthy of further studing.