阿魏酸纳米结构脂质载体的构建与质量评价

Construction and quality evaluation of ferulic acid-loaded nanostructured lipid carriers

目的:制备阿魏酸纳米结构脂质载体(FA-loaded NLCs)并评价其质量。方法:采用热熔乳化-超声波法制备FA-loaded NLCs,以脂质浓度(X1),药物浓度(X2)和表面活性剂浓度(X3)作为考察因素,以平均粒径(Y1)和包封率(Y2)作为评价指标,通过Box-Behnken实验设计优化得到FA-loaded NLCs最优处方,按照最优处方制备3批FA-loaded NLCs并测定了粒径分布和包封率,并使用透射电镜观察FA-loaded NLCs的微观形态,并比较了阿魏酸(FA)乙醇溶液和FA-loaded NLCs在pH值为7.4的磷酸盐缓冲液(PBS)中的体外释药速率。结果:通过优化得到FA-loaded NLCs的最优处方为:脂质浓度为2.7%,药物浓度为69.6mg/mL,表面活性剂浓度为3%,FAloaded NLCs均呈淡蓝色透明状液体,粒径大小为(167.6±34.6)nm,包封率为(81.5±3.6)%;通过透射电镜可观察到FA-loaded NLCs呈类球形分布,大小均匀;FA乙醇溶液在pH值7.4的PBS中释药较快,而FA-loaded NLCs释药缓慢,说明NLCs可以减缓FA的释药速率。结论:本研究通过Box-Behnken实验设计方法成功制备了FA-loaded NLCs,处方设计合理,工艺可行。

Objective:To prepare ferulic acid-loaded nanostructured lipid carriers(FA-loaded NLCs)and evaluation of their quality.Methods:FA-loaded NLCs were prepared by hot melt emulsification ultrasonic method.The lipid concentration(X1),drug concentration(X2)and surfactant concentration(X3)were used as the investigation factors,with the average particle size(Y1)and the encapsulation efficiency(Y2)as the evaluation index,the optimal formulation of FA-loaded NLCs was obtained through Box-Behnken experiment design.The FA-loaded NLCs were prepared according to the optimal formulation and the particle size distribution and entrapment efficiency were measured.The morphology of FA-loaded NLCs was observed by transmission electron microscopy.The in vitro release rate of FA ethanol solution and FA-loaded NLCs in pH 7.4 PBS was compared.Results:The optimal formulation of FA-loaded NLCs was optimized as follows:lipid concentration 2.7%,drug concentration 69.6mg/mL,surfactant concentration 3.0%.The FA-loaded NLCs were light blue transparent liquid with particle size of(167.6±34.6)nm,encapsulation efficiency(81.5±3.6)%.The FA-loaded NLCs were observed to be spherically distributed and uniform in size by transmission electron microscopy.The FA ethanol solution released faster in pH 7.4 PBS,while FA-loaded NLCs released slowly.Conclusion:In this study,Box-Behnken experimental design method has successfully developed FA-loaded NLCs.The formulation design is reasonable and the process is feasible.It is worth further research and development.