氯硝柳胺乙醇胺盐纳米剂的制备与杀螺效果  

Preparation of niclosamide ethanolamine nano-suspension and its molluscicidal effect

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

机构地区：[1]东南大学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

出　　处：《中国血吸虫病防治杂志》2007年第2期102-106,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：目的制备氯硝柳胺乙醇胺盐纳米剂并观察其杀螺效果。方法氯硝柳胺乙醇胺盐和高分子稳定剂聚乙烯吡咯烷酮（PVP）一起溶于二甲亚砜中制成原液，快速搅拌下加入到水中迅速分散，氯硝柳胺乙醇胺盐快速析出成为纳米颗粒，为稳定的溶胶体系，观察工艺条件与氯硝柳胺乙醇胺盐纳米剂颗粒粒径和稳定性的关系及杀螺效果。同时，对纳米制剂进行实验室浸杀试验、现场浸杀试验和现场喷洒杀螺试验。结果当稳定剂PVP K17与药物的质量比在1：2～1：3范围内时，稳定剂能起到较好的结晶阻拒作用，使纳米溶胶体系稳定，得到氯硝柳胺乙醇胺盐纳米颗粒的平均粒径约100nm，存放1个月不析出；快速搅拌制备的纳米颗粒细小而稳定。实验室浸杀试验纳米剂的有效药物浓度为氯硝柳胺乙醇胺盐可湿性粉剂（WPN）的1／2时，其杀螺效果与WPN杀螺效果相当；现场浸杀试验和现场喷洒杀螺试验中纳米剂的有效药物浓度为WPN的1／5时，其杀螺效果与WPN杀螺效果相当。结论氯硝柳胺乙醇胺盐纳米剂是一种杀螺作用强、使用方便的新颖杀螺剂型，值得进一步推广应用。Objective To prepare a novel nano-suspension of niclosamide ethanolamine and evaluate its molluscicidal effect. Methods Niclosamide ethanolamine and stabilizing agent——polyvinylpyrrolidone （PVP） were dissolved in dimethyl sulfoxide. After the solution was added into water under fast stirring, niclosamide ethanolamine was quickly precipitated to form nanoparticles and nano-suspension was obtained. The weight ratio of PVP to niclosamide ethanolamine, concentration, temperature, stirring speed on the size and distribution of the nanoparticles were investigated. The moUuscicidal effect of niclosamide ethanolamine nano-suspension was measured by immersion and spray methods in the laboratory and field. Results When the weight ratio of PVP to niclosamide ethanolamine was from 1 ： 2 to 1 ： 3, the nanoparticles of the niclosamide ethanolamine had diameters about 100 nm and the nano-suspension was stable without agglomerating for more than 1 month; as the speed of the stirring increased, the nanoparticles prepared became smaller and more stable. LC50 of the nano-suspension was 0. 054 4 mg/L but the LC50 of wettable powder of nielosamide ethanolamine salt （WPN） was 0. 125 0 mg/L. In the field immersion and spray tests, the concentration of nano-suspension as only 1/5 of active content of WPN achieved the same molluscicidal effect with WPN. Conclusions The nano-suspension has higher molluscicidal effect than WPN and the novel formulation of nielosamide has more advantages than WPN, it is useful for snail control in the field.

关 键 词：剂氯硝柳胺乙醇胺盐 纳米 稳定剂 杀螺效果 

分 类 号：R383.24[医药卫生—医学寄生虫学]