去甲斑蝥素聚乳酸-聚乙二醇纳米粒的制备及细胞毒性实验  

Preparation and cytotoxicity of polylactic acid-polyethylene glycol nanoparticles loaded with norcantharidin

作　　者：任杰[1] 仲谦[1] 李航[1] 袁华[1] 郁晓[1] 成浩[1] 

机构地区：[1]同济大学材料科学与工程学院纳米与生物高分子材料研究所,上海200092

出　　处：《药学服务与研究》2007年第4期294-297,共4页Pharmaceutical Care and Research

基　　金：上海市科委纳米专项课题资助项目(No.0452nm059)

摘　　要：目的:制备去甲斑蝥素纳米粒(norcantharidin nanoparticles,NCTD-NP),并考察其缓释特性和细胞毒性。方法:以聚乳酸-聚乙二醇为载体,采用相分离法制备NCTD-NP。用激光粒度仪测定纳米粒的粒径,以透射电镜观察其形态,以HPLC法测定其包封率,以紫外分光光度法考察其体外释放特性。应用四甲基偶氮唑盐微量酶反应比色法(MTT法)比较NCTD-NP和NCTD对胆囊癌GBC-SD细胞的细胞毒性。结果:纳米粒的粒径为(97.4±14.5)nm,表面光滑,包封率为(51.7±1.32)%,具有良好缓释性能。相同浓度的NCTD-NP和NCTD的细胞毒性在24 h之前基本相同,但NCTD-NP对GBC-SD细胞的生长有更持久的抑制效果,在IC50浓度48 h时仍抑制(56.42±9.45)%,而NCTD组仅抑制(23.14±3.77)%,两组有显著差异(P<0.01)。结论:NCTD-NP具有良好的缓释性能,并且可较长时间抑制胆囊癌GBC-SD细胞的生长。Objective： To prepare norcantharidin nanoparticles（NCTD-NP） and investigate their sustained-release property and cytotoxicity. Methods： NCTD-NP were prepared by phase separation method, using polylactic acid-polyethylene glycol （PLA-PEG） as carrier. Laser light scattering technique was used to determine size of the nanoparticles. The morphology of NCTD-NP was assayed by transmission electron microscopy （TEM）. The entrapment ratio and release characteristics in vitro of NCTD-NP were measured by HPLC method and ultraviolet spectrophotometry, respectively. The effect of NCTD-NP and NCTD on the invasion of GBC-SD cell lines of human gallbladder carcinoma was studied by methyl thiazolyl tetrazolium （MTT） method. Results： The grain size of NCTD-NP was （97.4±14.5） nm with the entrapment rate of （51.7±1.32）%. NCTD-NP possessed good sustained-release property in contrast to the naked drug. In the cell experiment, the in vitro inhibition rate of GBC-SD cell growth was similar between NCTD-NP and NCTD at same concentration before 24 h. However, the growth of GBC-SD cell lines was inhibited for longer time in NCTD-NP group than that in NCTD group. The inhibition rate of GBC-SD cell lines at 48 h was （56.42 ± 9.45）% in NCTD-NP group and （23. 14 ±3. 77）% in NCTD group when the drug concentration was IC50. There was significant difference between the two groups （P〈0. 01）. Conclusion： NCTD-NP show advantage in sustained-release and can effectively inhibit the growth of GBC-SD cell for 48 h.

关 键 词：去甲斑蝥素 纳米颗粒 制备 细胞毒性 聚乳酸 聚乙烯二醇类 

分 类 号：R979.1[医药卫生—药品] R944.9[医药卫生—药学]