Preparation and antitumor activity evaluation of self-assembled nanoparticles of diosgenin derivative
OBJECTIVE To explore the antitumor activity of diosgenin derivative and docosahexaenoic acid(DGG/DHA)self-assembled nanoparticle DDHs modified by hyaluronic acid(HA)in vitro.METHODS DGG/DHA were mixed in equal proportions and dual-drug self-assembled nanoparticle was prepared by the nanoprecipitation.The self-assembled nanoparticle DDHs were modified and characterized by HA.The preparation characteristics were summarized,including particle size,Zeta potential,stability and safety.The inhibitory activities of DDHs on A549,HepG-2,SMMC-7721,MCF-7,4T1 and MGC can-cer cells were examined by CCK-8 assay.Cellular uptake of DDHs in MGC was further studied.RESULTS DDHs modified by HA became smooth and stable.The average particle size of DDHs was(196.8±3.1)nm,PDI(0.158±0.01)and Zeta poten-tial-(30.73±0.76)mV.The stability of DDHS was decent and hemolytic activity of DDHs was significantly lower than that of nanoparticles without HA surface modification at normal pH value.DDHs showed a dose-dependent inhibition in the growth of A549,HepG-2,SMMC-7721,MCF-7,4T1 and MGC.As compared with DGG and DHA alone,DDHs showed synergistic effect against cancer cells with synergistic indices＜1.DDHs showed a higher cellular uptake in human gastric cancer cells.CONCLUSION Self-assembled nanoparticles modified by HA have a small particle size and decent profiles of stability and safety.HA modified self-assembled nanoparticle DDHs have exhibited strong inhibitory effect on cancer cell lines with an excel-lent synergistic effect.
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