三氧化二砷纳米粒的制备及对4种肿瘤细胞的抑制作用

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。

Preparation of Arsenic Trioxide Nanoparticles the Cytotoxicity against Four Tumor Cells

OBJECTIVE To prepared arsenic trioxide solid liguid nanoparticles with central composite design and study the inhibitory effect of arsenic trioxide solid liqid nanoparticles on four kinds of tumor cells. METHODS Arsenic trioxide solid lipid nanoparticles were prepared by emulsion-ultrasonic dispersion method. And MTT experiment was used to investigate the inhibition of four tumor cells. RESULTS The optimal formulation was screened as monostearin 0.11 g and soy lecithin 0.18 g. Average size of nanoparticles was 131.54 nm. Encapsulation efficiency was 73.46% and drug loading was 1.07%. The proliferations of four cells were inhibited by different concentrations of arsenic trioxide. And nanoparticles further induced the apoptosis of cells. CONCLUSION Arsenic trioxide solid lipid nanoparticles prepared by emulsion-ultrasonic dispersion method owned well stability and uniformity of particle distribution which meets pharmaceutical requirement. The inhibitory effect of arsenic trioxide solid lipid nanoparticles carrying cationic potential is the most notable.