目的 制备布雷菲德菌素A固体脂质纳米粒(brefeldin a solid lipid nanoparticles,BFA-SLNs),并评价其体外抗肿瘤效果。方法 采用超声分散法制备BFA-SLNs,正交试验优化处方。测定其平均粒径、多分散指数、Zeta电位、载药率、包封率和体外释放度。采用CCK-8法评价其体外对肝癌细胞HepG2的增殖抑制作用。结果 激光纳米粒度仪测定其平均粒径为(185.38±4.74) nm,多分散指数为(0.233±0.03),Zeta电位为(-66.10±2.26) mV,载药率为(7.64±0.28)%,包封率在80%以上,在体外释放度试验中表现出良好的缓释作用。BFA-SLNs对HepG2细胞有较强的增殖抑制作用。结论 制备得到的BFA-SLNs粒径均一,分散性良好,包封率较高且具有缓释作用,体外抗肿瘤效果较游离药物强。
Abstract
OBJECTIVE To prepare brefeldin A solid lipid nanoparticles (BFA-SLNs) and evaluate its antitumor effect in vitro. METHODS BFA-SLNs was prepared by ultrasonic dispersion method, and the formulation was optimized by orthogonal test. The average particle size, polydispersity index (PDI), Zeta potential, loading efficiency (LE), entrapment efficiency (EE) and release effect in vitro were determined. CCK-8 method was used to evaluate its inhibitory effect on the proliferation of HepG2 cells in vitro. RESULTS According to the results of laser nano particle size analyzer, the average diameter, PDI and Zeta potential were (185.38±4.74) nm, (0.233±0.03), (-66.10±2.26) mV, respectively. The LE% was (7.64±0.28)%. The EE% was more than 80%. It has a good sustained-release effect in vitro release test. BFA-SLNs can effectively inhibit the proliferation of HepG2 cells. CONCULUSION BFA-SLNs has high EE and sustained-release effect, and its anti-tumor effect is stronger than that of free drug in vitro.
关键词
布雷菲德菌素A /
固体脂质纳米粒 /
超声分散法 /
正交试验 /
抗肿瘤活性
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Key words
brefeldin A /
solid lipid nanoparticle /
ultrasonic dispersion method /
orthogonal test /
antitumor activity
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中图分类号：
R944
R969
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参考文献
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脚注
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基金
国家自然科学基金项目资助(21764016)
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