Preparation of chitosan/isoliquiritigenin nanoparticles and their inhibitory effects on the proliferation of human lung cancer cell line A549

doi:10.3969/j.issn.2095-4344.1360

Abstract

Abstract:

BACKGROUND: Isoliquiritigenin, one kind of isoflavone compounds, has a wide range of biological activities, such as anti-cancer, anti-virus, and anti-diabetes, but its clinical application is limited by its poor water solubility.

OBJECTIVE: To prepare chitosan/isoliquiritigenin nanoparticles and investigate their inhibitory effects on human lung cancer cell line A549 in vitro.

METHODS: The chitosan/isoliquiritigenin nanoparticles were prepared by ionic gelation method with chitosan as the carrier material, isoliquiritigenin as the model drug, and sodium tripolyphosphate as the ionic crosslinking agent. The nanoparticle size, dispersion, and Zeta potential were investigated by malvern laser particle size analyzer. The morphology of the nanoparticles was observed by transmission electron microscopy. The encapsulation efficiency and cumulative release rate of the nanoparticles were measured by centrifugation. Isoliquiritigenin and chitosan/isoliquiritigenin nanoparticles were placed in dialysis bags and their dynamic release was determined in PBS buffer. Human lung cancer cell line A549 was cultured in different concentrations (1, 5, 25 mg/L) of isoliquiritigenin, chitosan/isoliquiritigenin nanoparticles, and chitosan nanoparticles. MTT assay was used to investigate the inhibitory effects of chitosan/isoliquiritigenin nanoparticles on human lung cancer cell A549 in vitro after 48 hours of culture. The growth-inhibitory rate was calculated.

RESULTS AND CONCLUSION: The chitosan/isoliquiritigenin nanoparticles were spherical or quasi spherical in shape with complete structure and of relatively uniform size. The average particle size, dispersion and Zeta potential of chitosan/isoliquiritigenin nanoparticles were (159±20) nm, 0.243 and +17.2 mV, respectively. The encapsulation efficiency and cumulative release rate of the nanoparticles were (85.28±1.31)% and (13.28±0.53)% respectively.The release of free isoliquiritigenin was completed within 8 hours, while the chitosan/isoliquiritigenin nanoparticles had sustained release property in vitro, with 72-hour cumulative release amount of 83.98%. This well fitted the first-order kinetic model. Chitosan nanoparticles at different concentrations had no inhibitory effects on the growth of A549 cells. Both isoliquiritigenin and chitosan/isoliquiritigenin nanoparticles inhibited the growth of A549 cells in a concentration-dependent manner, and the inhibitory effect of chitosan/isoliquiritigenin nanoparticles was stronger than that of isoliquiritigenin when used at the same concentration (P < 0.05). The results suggest that the chitosan/isoliquiritigenin nanoparticles prepared by ionic crosslinking method had encouraging sustained release performance and enhanced the inhibitory effects of isoliquiritigenin on the proliferation of A549 cells in vitro.

Key words: isoliquiritigenin, chitosan, nanoparticle, ionic crosslinking method, tumor, A549, cell proliferation, inhibitory effect

CLC Number:

Lü Wenjuan, Liu Fuding, Wang Taojiao, Wan Lang, Chen Fang. Preparation of chitosan/isoliquiritigenin nanoparticles and their inhibitory effects on the proliferation of human lung cancer cell line A549[J]. Chinese Journal of Tissue Engineering Research, 2019, 23(26): 4200-4205.

Figures/Tables 5

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