Abstract

Objective To prepare active and controlled paclitaxel-loaded nanoparticles, and to determine their effect on hepatocellular carcinoma HepG2 and Huh-7 cells. Methods The poly (D, L-lactide-co-glycolide) nanoparticles containing paclitaxel were prepared by o/w emulsification-solvent evaporation method. The drug encapsulation efficiency, loading efficiency and release profile rate in vitro were measured by high-performance liquid chromatography. The morphology and size of nanoparticles were observed by scanning electron microscopy and particle size analyzer, respectively. Hepatocellular carcinoma HepG2 and Huh-7 cells were co-cultured with paclitaxel nanoparticles, and the changes of cell morphology were observed by inverted microscope, and the cell viability was examined by the methyl thiazolyl tetrazolium assay. Results The nanoparticles were spherical shape with particle size 216 nm, and the drug encapsulation efficiency and loading efficiency was 87.4% and 1.79%, respectively. The drug release pattern showed an early burst release followed by a slow sustained release. Released drug from paclitaxel-loaded nanoparticles resulted in injury of HepG2 and Huh-7 cells. At 1, 2, 3 and 5 days after administration, the survival rates of HepG2 cells co-cultured with paclitaxel nanoparticles were (76.6±5.1)%, (57.3±4.9)%, (29.7±4.4)%, and (7.2±2.0)%, respectively, and the survival rates in the blank group were (94.3±6.8)%, (91.0±6.6)%, (90.7±5.6)%, and (87.4±5.7)%; the survival rates of Huh-7 cells were (82.1±8.0)%, (63.5±5.6)%, (40.2±3.9)%, and (11.4±3.6)%, respectively, and the survival rates in the blank group were (93.5±7.7)%, (92.5±6.8)%, (89.0±6.2)%, and (86.1±6.5)%. The survival rate of cells co-cultured with paclitaxel nanoparticles was lower than that of the blank group (all P < 0.05), and the cell survival rate showed a decrease change with prolonged co-cultured time (both P < 0.05). Conclusion Paclitaxel nanoparticles could play an anti-tumor effect on hepatocellular carcinoma HepG2 and Huh-7 cells in vitro in a controlled manner, providing a new dosage form for the clinical application of anti-hepatoma drugs. Key words: Nanoparticle; Paclitaxel; Liver neoplasms; Drug delivery

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