去甲斑蝥素纳米胶束的制备及抑瘤作用研究

发布时间：2018-01-15 10:46

本文关键词：去甲斑蝥素纳米胶束的制备及抑瘤作用研究　出处：《中国药房》2017年19期 　论文类型：期刊论文

【摘要】：目的:制备去甲斑蝥素纳米胶束,并研究其抑瘤作用。方法:采用三嵌段共聚物二硬脂酰磷脂酰乙醇胺-聚乙二醇-马来酰亚胺在水中自组装形成去甲斑蝥素纳米胶束。观察所制纳米胶束形态,考察其载药率、包封率、粒径和Zeta电位。通过MTT法考察阴性对照组(磷酸盐缓冲液)、载体组(空白纳米胶束)、阳性对照组(去甲斑蝥素原料药,5~320μg/m L)和去甲斑蝥素纳米胶束组(以去甲斑蝥素计,5~320μg/m L)人肺癌A549细胞在作用不同时间(24、48、72 h)后的细胞生存率。将荷瘤裸鼠随机分为空白对照组、去甲斑蝥素注射液组(1 mg/kg)和去甲斑蝥素纳米胶束低、高剂量组(0.5、1 mg/kg),每组6只,每天尾iv相应药物1次,连续8周;每周测量肿瘤的大小,给药结束后第2天检测瘤质量。结果:去甲斑蝥素纳米胶束呈圆球状,载药率为(2.82±0.05)%,包封率为(83.67±1.78)%,粒径为(138.6±45.8)nm,Zeta电位为-(12.75±0.34)m V(n=6);载体组A549细胞生存率无明显变化,阳性对照组和去甲斑蝥素纳米胶束组A549细胞生存率明显降低,与浓度和时间呈正相关,且去甲斑蝥素纳米胶束组细胞生存率降低程度较阳性对照组更明显(P0.01)。与空白对照组比较,3个给药组裸鼠的瘤质量均减小(P0.05),其中去甲斑蝥素纳米胶束高剂量组减小程度较去甲斑蝥素注射液组更明显(P0.05)。结论:成功制得去甲斑蝥素纳米胶束,其对A549细胞具有较好的体内外抑瘤作用。
[Abstract]:Objective: to prepare norcantharidin nano-micelles. Methods: the nanomicelles of norcantharidin were self-assembled in water with triblock copolymers of distearylphosphatidyl ethanolamine-polyethylene glycol-Maleimide. The drug loading rate, encapsulation efficiency, particle size and Zeta potential were investigated by MTT. The negative control group (phosphate buffer solution, carrier group (blank nano-micelle), positive control group (norcantharidin raw drug) was investigated by MTT method. Human lung cancer cell line A549 was treated with 5 渭 g / m L of norcantharidin and 5 渭 g / m L of norcantharidin at different time points. The tumor bearing nude mice were randomly divided into control group, norcantharidin injection group (1 mg / kg) and norcantharidin nano-micelle low, high dose group (0.5 mg / kg). 1 mg / kg, 6 rats in each group, the corresponding drugs were given at the end of the day for 8 weeks; The tumor size was measured weekly, and the tumor quality was detected on the second day after administration. Results: norcantharidin nanoparticles were spherical in shape, and the drug loading rate was 2.82 卤0.05%. The entrapment efficiency was 83.67 卤1.78 and the Zeta potential was -12.75 卤0.34 ~ 0.34 m ~ (-1) 路m ~ (-1) ~ (-1) ~ (-1) ~ (-1) ~ (-1) ~ (-1) ~ (-1) ~ (-1) ~ (-1) ~ (-1) ~ (-1). The survival rate of A549 cells in carrier group had no significant change. The survival rate of A549 cells in positive control group and norcantharidin nano-micelle group was significantly decreased, which was positively correlated with the concentration and time. The cell survival rate in the norcantharidin nano-micelle group was significantly lower than that in the positive control group (P 0.01). Compared with the blank control group, the tumor mass of the nude mice in the three administration groups decreased significantly (P 0.05). The reduction of norcantharidin nano-micelle in high dose group was more obvious than that in norcantharidin injection group (P 0.05). Conclusion: norcantharidin nano-micelles were successfully prepared. It has a good inhibitory effect on A549 cells in vivo and in vitro.
【作者单位】：苏州卫生职业技术学院药学院;苏州大学医学部药学院;香港浸会大学中医药学院;
【基金】：江苏省卫生厅科技项目(No.JZ201402)
【分类号】：R943;R96
【正文快照】： 去甲斑蝥素(Norcantharidin)是将斑蝥属昆虫南方大斑蝥和黄黑小斑蝥的虫体所含的抗癌有效成分斑蝥素(Cantharidin)1,2位去甲基而得的,是我国首先研制开发的具有一定潜力的抗肿瘤药物[1-2]。但由于其毒性很大,在人工胃液及人工肠液中以去甲斑蝥酸的形式存在[3-4],水溶性增加,导

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