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目的采用星点设计优化处方,制备三氧化二砷固体脂质纳米粒并探讨其对4种肿瘤细胞的抑制作用。方法采用乳化超声法制备三氧化二砷固体脂质纳米粒。采用MTT法考察三氧化二砷固体脂质纳米粒对4种肿瘤细胞的体外抑制作用。结果筛选的最优处方为PEG-单硬脂酸甘油酯用量0.11 g,大豆卵磷脂的用量0.18 g。平均粒径为131.54 nm,包封率73.46%,载药量为1.07%。不同浓度三氧化二砷固体脂质纳米粒对4种细胞均有抑制增殖作用。结论采用乳化超声法制得的三氧化二砷固体脂质纳米粒具有较好的稳定性,粒子分布均匀,符合制剂学要求。携带阳离子三氧化二砷固体脂质纳米粒组抑制作用最强。
Objective To optimize the prescription by using the star point design and prepare solid lipid nanoparticles of arsenic trioxide and investigate its inhibitory effects on four kinds of tumor cells. Methods The arsenic trioxide solid lipid nanoparticles were prepared by emulsification ultrasound. MTT assay of arsenic trioxide solid lipid nanoparticles on four kinds of tumor cells in vitro inhibition. Results The optimal prescription for screening was 0.11 g PEG-monostearate and 0.18 g soy lecithin. The average particle size was 131.54 nm, the entrapment efficiency was 73.46% and the drug loading was 1.07%. Different concentration of arsenic trioxide solid lipid nanoparticles inhibited the proliferation of all four kinds of cells. Conclusion The solid nanoparticles of arsenic trioxide obtained by emulsified ultrasound have good stability and uniform distribution of particles, which meets the formulation requirements. Carrying cationic arsenic trioxide solid lipid nanoparticles group the strongest inhibition.