地克珠利纳米脂质体的研制及表征

Development and physicochemical characterization of diclazuril nanoliposomes

地克珠利(Diclazuril,DIC)是广泛应用于畜禽养殖业中球虫病防治的一种经典抗球虫药物。本研究旨在采用薄膜冻融法制备地克珠利纳米脂质体,以地克珠利纳米脂质体的包封率为评价指标进行单因素考察,通过正交试验确定最佳制备条件,并对在最佳条件下制备的地克珠利纳米脂质体进行表征考察。最终确定地克珠利纳米脂质体最佳制备条件为:药物与卵磷脂质量比为1∶30,卵磷脂与胆固醇质量比为4∶1,水合介质pH为7.0,水合温度为55℃,水合时间1.5 h,冻融次数为3次。利用最佳条件制备得到的地克珠利纳米脂质体平均包封率为92.23%±0.57%。地克珠利纳米脂质体的表征结果显示,脂质体在透射电镜下呈均一的球形或近球形结构,平均粒径为117.2 nm±1.2 nm,PDI平均值为0.147±0.004,Zeta电位值为-47.37 m V±0.67 m V,表明纳米脂质体粒径小且分布均一,稳定性试验结果显示,地克珠利纳米脂质体宜在4℃条件下避光储存。本研究制备出了一种包封率高、稳定性好的地克珠利纳米脂质体,为地克珠利在兽医临床上的使用提供了新的方法。

Diclazuril(DIC) is a classic anticoccidial drug widely used in the prevention and control of coccidiosis in livestock and poultry breeding.The purpose of this study is to prepare diclazuril nanoliposomes using freeze-thaw method.By single factor and orthogonal tests analysis,the encapsulation rate of diclazuril nanoliposomes was used as the indicator for screening the optimal preparation conditions.Physicochemical characterization of diclazuril nanoliposomes prepared under the optimal preparation condition were evaluated.The results showed that the optimal preparation conditions of diclazuril nanoliposomes were as follows:the mass ratio of drug to lecithin was 1∶30,the mass ratio of lecithin to cholesterol was 4∶1,the p H of the hydration medium was 7.0,and the hydration temperature was 55 ℃.The hydration time is 1.5 h,and the number of freeze-thaw cycles is 3 times.The average encapsulation efficiency of diclazuril nanoliposomes prepared under optimal conditions is 92.23%±0.57%.The characterization results of diclazuril nano-liposomes showed that the liposomes had a uniform spherical or nearly spherical structure under the transmission electron microscope.The average particle size of diclazuril nanoliposomes was 117.2 nm±1.2 nm and the average polymer dispersity index(PDI) was 0.147±0.004.The Zeta potential was-47.37 m V±0.67 m V.Results of physicochemical characterization showed that dicclazuril nanoliposomes had small particle size and uniform distribution.The stability test results showed that diclazuril nanoliposomes were best stored at 4 ℃under dark conditions.In conclusion,this study prepared diclazuril nanoliposomes with high encapsulation efficiency and good stability,which provided a new method for the use of diclazuril in veterinary clinic.