Top-down方法制备氯硝柳胺纳米剂的研究  

Preparation of niclosamide nanoparticle by the method of Top-down

作　　者：郭峰[1] 姜柳[1] 李新松[1] 戴建荣[2] 朱荫昌[2] 

机构地区：[1]东南大学化学化工系生物材料和药物释放实验室,南京210018 [2]江苏省血吸虫病防治研究所,江苏省寄生虫分子生物学重点实验室,江苏省寄生虫病学重点学科

出　　处：《中国血吸虫病防治杂志》2006年第6期411-415,共5页Chinese Journal of Schistosomiasis Control

基　　金：国家高技术研究发展计划(863计划)(2004AA2Z3540)

摘　　要：目的研制氯硝柳胺纳米剂。方法将氯硝柳胺与各种助剂和水按一定的比例混合,选择适当的球磨条件,用行星式球磨机进行研磨,用光学显微镜和激光粒度仪评价所得到的纳米剂。结果使用行星式球磨方法,选用大球料比、高转速、长时间的高能量球磨条件,可提高球磨效果;在表面活性物质、消泡剂和助磨剂存在的条件下,加入亲水高分子物质可对氯硝柳胺的颗粒起到保护作用。实验配方为氯硝柳胺25%(质量比,下同)、吐温-8010%、甲基硅油5%、二氧化硅10%、聚氧乙烯10%时,在转速为600r/min、球料比为20∶1的球磨条件下,预磨20h后用1mm锆球研磨至100h,可得到粒径分布最大值(DMax)为71nm、50%粒子的粒径(D50)为81nm、90%粒子的粒径(D90)为164nm的纳米粒子,形成稳定、易于分散的氯硝柳胺纳米液。结论用行星式球磨方法,在亲水高分子的保护下,选用高能量球磨条件,可得到稳定的氯硝柳胺纳米剂。Objective To develop the nanoparticle of niclosamide. Methods Niclosamide was milled by a planet ball mill set ,mixed with different amounts of additives and water. The nanopar ticle of niclosamide was obtained at proper ball milling condition,which was characterized by micro scope,laser particle analyzer. Results High ratio of mass of ball to materials,high rotating speed and long-time improved ball-milling effect using planet ball milling method. At the presence of sur factant, antifoaming agents and other additives,addition of hydrophilie polymeric material improved protective effect on niclosamide nanoparticles. With the formulation of 25 % of noelosamide, 10% of Tween-80,5 % of methyl silicone oil, 10% of silicon dioxide, 10% of polyethylene oxide,the rotating speed of 600 r/min and 20 ; 1 of the ratio of ball to material, nanoparticles of niclosamide can be obtained by milling for 80 hours with 1 mm Zirconium balls after pre-milling for 20 hours with 8 mm and 4 mm balls. The nanoparticles had DMAX of 71 nm, D50 of 81 nm,D90 of 164 nm. The solution was stable and easily dispersed. Conclusion Under the protection of hydrophilie polymers,stable nanopartiele solution of nielosamide can be prepared by the method of planet ball-milling choosing high-energy ball-milling condition.

关 键 词：氯硝柳胺 纳米粒子 Top—down方法 

分 类 号：TQ453.21[化学工程—农药化工] R383.24[医药卫生—医学寄生虫学]