王红娟 王芳 王亚桃

摘要 目的：为了得到苍耳子油脂质体的最佳制备工艺。方法：以卵磷脂和胆固醇为膜材，采用薄膜分散水化法制备脂质体，利用游离药物与含药脂质体的重量差异通过超速离心法分离，并计算其包封率。根据单因素实验得对其包封率有显著影响的因素，以正交试验设计筛选出制备脂质体的最佳制备方法。结果：通过正交试验得到最优方法为：卵磷脂：胆固醇3∶1、苍耳子油：卵磷脂1∶7、水化溶液体积20 mL，此条件下测得其包封率为68.0%。结论：该方法所得脂质体包封率达60%以上，比较稳定。

关键词 苍耳子油;脂质体;包封率;正交试验

Study on Preparation Technology of Xanthii Fructus Oil Liposomes

WANG Hongjuan，WANG Fang，WANG Yatao

（Gansu Medical College，Pingliang 744000，China）

Abstract Objective：In order to obtain the optimal preparation process of Xanthii Fructus oil liposomes.Methods：Lecithin and cholesterol was used as membrane materials，liposomes were prepared by a thin film dispersion hydration method.The weight difference between free drugs and drug-containing liposomes was used to separate them by ultracentrifugation，and their encapsulation rates were calculated.According to the single factor experiment，the factors that have a significant effect on its encapsulation efficiency were obtained.The best method for preparing liposomes was screened by orthogonal test design.Results：The optimal method obtained through orthogonal test was：lecithin：cholesterol 3∶1，Xanthii Fructus oil：lecithin 1∶7，and the volume of the hydration solution was 20 mL.Under this condition，the encapsulation rate was 68.0%.Conclusion：The encapsulation rate of liposomes obtained by this method is more than 60%，which is relatively stable.

Keywords Xanthii Fructus Oil; Liposome; Encapsulation efficiency; Orthogonal test

中图分类号：R283文献标识码：Adoi：10.3969/j.issn.1673-7202.2021.02.007

苍耳子为菊科植物苍耳（Xanthium sibiricum Patr.et Widd.）干燥成熟带总苞的果实，其中油脂是苍耳子的主要成分，油脂中主要含有酚酸类成分，如绿原酸、异绿原酸A、异绿原酸C等[1]。现代药理研究表明苍耳子具有抗菌、抗病毒、抗炎、镇痛、降血糖、抗过敏等作用且对鼻炎具有很好的疗效[2-4]。脂质体是一种具有类似生物膜的双分子层结构的超微球形载体制剂，它主要用于药物的制备，即利用脂质体溶于细胞膜的性质，将药物送入细胞内部，保护定向至某治疗的靶器官或组织中[5-7]，因此脂质体作为鼻腔给药的一种新型剂型其具有以下优点：将药物包封入脂质体后鼻腔给药，不仅能有效地减少药物对鼻腔的刺激性和毒性，增加药物疗效，并可使药物通过磷脂双分子层幻世控制释放，克服以往气雾剂吸收快及必须频繁给药的缺陷[8-9]。……