摘要
[目的]优化多杀霉素/壳聚糖微球的制备条件,并初步探究其在不同温度下的释药行为。[方法]采用均相沉淀法制备多杀霉素/壳聚糖微球。通过测定微球在不同温度下的溶胀度和累积释药率,研究其药物释放温敏性。[结果]微球适宜制备条件:壳聚糖水溶液1%,多杀霉素甲醇溶液1.5%,壳聚糖与多杀霉素的质量比2∶1,乳化剂吐温80 5%,15 000 r/min下剪切3 min,沉淀剂为3%的氨水和异丙醇的混合液(体积比4∶1),加入量为壳聚糖溶液与多杀霉素甲醇溶液总体积的60%。微球包封率大于90%,载药量大于30%,中粒径D_(50)为40μm左右。在pH值6.86的缓冲溶液中,微球的溶胀度、释药速率和累积释药率均随着温度的升高而升高,表现出明显的温度敏感性。[结论]多杀霉素/壳聚糖微球有望开发为温度响应型环境友好控释制剂。
[Aims ] The aims were to optimize the preparation conditions of spinosad/chitosan microspheres and preliminarily explore the drug release behavior at different temperatures.[Methods ] Adopting homogeneous precipitation method, the spinosad/chitosan microspheres were prepared. The temperature sensitivity of drug release was studied by determining the swelling ratio and the cumulative release amount of the microspheres at different temperatures.[Re s ults ] The optimal preparation conditions were: the ratio of chitosan and spinosad is 2∶1 (by mass), the concentration of emulsifier Tween 80 is 5%, the chitosan aqueous solution (1.0%) and spinosad methanol solution (1.5%) are mixed at the shear emulsifying of 15 000 r/min for 3 min, the precipitation reagent is the mixture solution of ammonia aqueous (3%) and isopropanol (4∶1, by vol), the volume of precipitation reagent is 60% of the total volume of spinosad methanol solution and chitosan aqueous solution. Under these conditions, the encapsulation efficiency of the microspheres was above 90%, the drug loading is above 30%, the median particle size D50 is about 40 μm. The swelling ratio, the release rate and the cumulative release amount were all increased with the temperature increased from 20 to 55 ℃, which shows apparently temperature sensitivity.[Conclusions ] The spinosad/chitosan microspheres are expected to be developed as an environmentally friendly controlled release formulation in response to temperature.
作者
王娟
李国宾
张保华
宋超
孔祥平
WANG Juan;LI Guo-bin;ZHANG Bao-hua;SONG Chao;KONG Xiang-ping(College of Chemistry and Pharmacy, Qingdao Agricultural University, Qingdao 266109, Shandong, China)
出处
《农药》
CAS
CSCD
北大核心
2019年第4期266-270,共5页
Agrochemicals
基金
国家自然科学基金(31501682)
山东省自然科学基金(ZR2014EL012)
青岛农业大学高层次人才科研基金(6631115037)
青岛农业大学大学生科技创新基金
关键词
多杀霉素
壳聚糖
均相沉淀
控释微球
温敏性
spinosad
chitosan
homogeneous precipitation
controlled release microspheres
temperature sensitivity
