依托泊苷固体脂质纳米粒的制备与抗癌活性研究  

Preparation and Antitumor Activity of Etoposide-loaded Solid Lipid Nanoparticles

作　　者：何瑶[1] 郭晓华[1] He Yao;Guo Xiaohua(Medical School, Xianyang Vocational College, Shaanxi Xianyang 712000, China)

机构地区：[1]咸阳职业技术学院医学院,陕西咸阳712000

出　　处：《中国药师》2018年第5期792-796,共5页China Pharmacist

摘　　要：目的:制备依托泊苷固体脂质纳米粒,并评价其对小鼠接种Lewis肺癌细胞的抑瘤率。方法:采用热熔乳化-高压均质法制备依托泊苷固体脂质纳米粒,考察依托泊苷固体脂质纳米粒的外观、微观结构、粒径分布、Zeta电位等理化性质,评价依托泊苷固体脂质纳米粒体外释药行为,比较依托泊苷固体脂质纳米粒与依托泊苷注射液对小鼠接种Lewis肺癌细胞的抑制效果。结果:本研究制备的依托泊苷固体脂质纳米粒外观呈淡蓝色透明状液体,在透射电镜观察呈圆整球状或类球状分布,大小较为均匀;平均粒径为(153.2±32.8)nm,Pd I为(0.185±0.031),Zeta电位为(-17.4±1.1)mV;依托泊苷固体脂质纳米粒可延缓药物释放,在24 h内药物累积释放52.4%;依托泊苷固体脂质纳米粒的抑瘤率显著高于依托泊苷注射液(P<0.05),说明依托泊苷固体脂质纳米粒能够显著抑制Lewis肺癌细胞在小鼠体内生长。结论:本研究通过热熔乳化-高压均质法制备的依托泊苷固体脂质纳米粒对Lewis肺癌细胞具有良好的抑瘤效果,可以作为依托泊苷的新型给药系统,对肺癌治疗具有一定的应用前景。Objective： To prepare solid lipid nanoparticles of etoposide and evaluate the inhibitory rate against Lewis lung cancer cells in mice. Methods： Etoposide-loaded solid lipid nanoparticles were prepared by a hot melting emulsification and high pressure homogenization method. The physicochemical properties such as the appearance, microstructure, particle size distribution and zeta potential of the solid lipid nanoparticles were studied. The in vitro release behavior of the solid lipid nanoparticles were evaluated. The inhibitory effect of etoposide-loaded solid lipid nanoparticles and etoposide injection on Lewis lung cancer cells was compared. Results ： Etoposide-loaded solid lipid nanopartieles showed a light blue transparent liquid, which was uniformly spherical under the transmission electron microscope. The average particle size was （153.2 ± 32.8） nm, PdI was （0. 185 ± 0.031 ） , and the zeta potential was （ - 17.4± 1.1 ） mV. The solid lipid nanoparticles could delay the drug release and 52.4% of the drug was released in 24 h. Etoposide-loaded solid lipid nanoparticles could significantly inhibit the growth of Lewis lung cancer cells in mice. And the inhibitory rate of the solid lipid nanoparticles was significantly higher than that of etoposide injection （P 〈 0.05）. Conclusion： The solid lipid nanoparticles prepared by hot melting emulsification and high pressure homogenization method have good antitumor effect on Lewis lung cancer cells, which can be used as a new drug delivery system for etoposide with certain application prospect in lung cancer treatment.

关 键 词：依托泊苷 固体脂质纳米粒 热熔乳化-高压均质法 抑瘤率 

分 类 号：R944.9[医药卫生—药剂学] R965.1[医药卫生—药学]