摘要
目的:制备姜黄素固体脂质纳米粒。方法:微乳法制备姜黄素固体脂质纳米粒。采用伪三元相图法优选微乳三相因素,确定优化条件后,将热微乳分散于冷水中制备固体脂质纳米粒。单因素试验初筛各因素(乳化剂、脂质材料、脂质用量、药脂比、冷水相温度和微乳保温温度)后,以包封率为指标进行正交试验优化处方,并进行验证试验。结果:65℃下由硬脂酸(油相)、聚山梨酯80(乳化剂)、乙醇(助乳化剂)组成三相,乳化剂与助乳化剂比为1∶4所制得的微乳最佳。固体脂质纳米粒的优化处方为姜黄素投药量为50 mg、硬脂酸的用量为0.5 g、冷水相温度为2℃、微乳保温温度为65℃;所得固体脂质纳米粒的包封率为87.73%、载药量为7.72%、粒径为(156.9±2.2)nm、多分散系数为0.480,平均Zeta电位为-24.8 m V(RSD<2%,n=3)。结论:采用微乳法制备固体脂质纳米粒操作简便、可行。
OBJECTIVE：To prepare the curcumin solid lipid nanoparticles.METHODS：Microemulsion method was adopted to prepare curcumin solid lipid nanoparticles（SLN） and pseudo-ternary phase diagrams was conducted to optimize the preferable three-phase microemulsion factors.The optimal conditions were determined,and then hot microemulsion was dispersed in cold water to prepare SLN.After the preliminary screening of the factors（emulsifiers,lipid materials,amount of lipids,drug-to-lipid ratio,cold water phase temperature and the holding temperature of microemulsion）by single-factor test,with the index of encapsulation efficiency,the orthogonal test was conducted to optimize the formulation,followed by the verification test.RESULTS：The best microemulsion was produced at 65 ℃ with three phases consisting of stearic acid（oil phase）,polysorbate 80（emulsifier）and ethanol（co-emulsifier）and the Kmratio of 1 ∶ 4.The optimal conditions for SLN were as follows as curcumin dosage of 50 mg,stearic acid of 0.5 g,cold water phase temperature of 2 ℃,holding temperature of microemulsion of 65 ℃.The encapsulation efficiency was 87.73% for solid lipid nanoparticles prepared,drug-loading rate was 7.72%,particle size was（156.9±2.2）nm,polydispersity coefficient was 0.480,average Zeta potential was-24.8 m V（RSD〈2%,n=3）.CONCLUSIONS：The microemulsion method to prepare SLN is simple and feasible.
出处
《中国药房》
CAS
北大核心
2015年第19期2698-2702,共5页
China Pharmacy
基金
天津市卫生局科技基金项目(No.2012KY32)
关键词
姜黄素
微乳法
固体脂质纳米粒
伪三元相图
包封率
正交试验
Curcumin
Microemulsion method
Solid lipid nanoparticles
Pseudo-ternary phase diagram
Encapsulation efficiency
Orthogonal test
