叶黄素自微乳的制备及质量控制

Preparation and Quality Control of Lutein Self-microemulsion

目的优选叶黄素自微乳制剂处方,并对优化后的处方进行质量评价。方法通过溶解度试验、单因素试验和星点-响应面设计等方法进行叶黄素自微乳制剂处方研究,采用马尔文粒径仪对自微乳的粒径和Zeta电位进行测定,采用溶出试验仪对叶黄素自微乳的体外溶出情况进行测试。结果优选出叶黄素自微乳的制剂处方为中链甘油三酯(MCT)30.00%、聚氧乙烯氢化蓖麻油(Cremophor RH40)41.37%、聚乙二醇-400(PEG-400)28.63%,该处方形成的自微乳液澄清透明,用水稀释后能很快形成澄清透明的微乳液,并可见该微乳液泛淡蓝色乳光;叶黄素在空白自微乳中的负载量为1 mg·g-1,负载叶黄素的自微乳稀释后形成橘黄色微乳液,其微乳液粒径为46.43 nm,Zeta电位为-5.07 mV,多分散系数PDI为0.10,表明微乳液的粒径分布均一。体外释放度试验中,叶黄素自微乳在10 min内可基本溶出,溶出百分比为67%左右。结论制备的叶黄素自微乳外观良好,性质稳定,遇水能形成纳米级别的微乳液,体外释放速度快,具有良好的应用前景。

OBJECTIVE To optimize the formulation of lutein self-microemulsion,and evaluate the quality of the obtained formulation.METHODS The lutein self-microemulsion was optimized by solubility experiment,single factor experiment and star-response surface design.The particle size and zeta potential was determined by the Malvern particle size analyzer,and the in vitro dissolution profile was tested by dissolution apparatus.RESULTS The optimized lutein self-microemulsion formulation was appeared as clear and transparent solution,composed of medium chain triglyceride(MCT)30.00%,polyoxyethylene hydrogenated castor oil(Cremophor RH40)41.37%,and polyethylene glycol-400(PEG-400)28.63%.When introduced to water under gentle agitation,a clear transparent microemulsion with light blue opalescence could be quickly formed.The loading amount of lutein in the blank self-microemulsion was 1 mg·g-1.The lutein-loaded self-microemulsion was diluted to form an orange microemulsion.The mean diameter,zeta potential,and polydispersity coefficient PDI was 46.43 nm,-5.07 mV,and 0.01,respectively,indicating that the microemulsion had a uniform particle size distribution.In the in vitro release test,lutein was substantially released from the self-microemulsion within 10 min,and the percentage of dissolution was about 67%.CONCLUSION The prepared lutein self-microemulsion has a good appearance and stable properties,and can form a nano-level microemulsion after diluted with water.It has a fast release rate in vitro,which provide a potential application prospect in the future.