摘要
目的制备黄芪甲苷纳米结构脂质载体(AST-NLC),初步研究其冻干工艺,并考察其理化性质。方法采用薄膜-超声分散法制备AST-NLC;选用不同冻干保护剂制备AST-NLC冻干粉末,以外观、色泽、再分散性、粒径和PDI为综合指标,优选保护剂的种类和浓度,拟定冻干工艺;考察AST-NLC的形态和冻干前后的粒径分布、Zeta电位、包封率及载药量。结果以10%的蔗糖作为冻干保护剂、-40℃超低温冰箱中预冻4 h后,迅速放入冷冻干燥机中冷冻干燥24 h,所得冻干粉末的外观、色泽、再分散性均较好;AST-NLC在透射电镜下呈球形;冻干前(后)的平均粒径为104.3±1.25 nm(144.1±17.08nm),PDI为0.118±0.033(0.132±0.055),Zeta电位为-7.00±0.35 mV(-11.2±0.9 mV),包封率为94.37%±0.39%(96.60%±0.45%),载药量为2.80%±0.02%(2.60%±0.05%)。结论所用AST-NLC的制备工艺简便,制得的AST-NLC包封率较高;采用优化后的冻干工艺可得到令人满意的AST-NLC冻干粉末。
OBJECTIVE To prepare and characterize the lyophilized Astragaloside IV-loaded nanostructured lipid carriers(AST-NLC).METHODS AST-NLC was prepared by film-ultrasound dispersion technique.The lyophilized AST-NLC were prepared using different supporting agent.The type and concentration of the supporting agents were optimized by the shape,color,redispersion,size and PDI of the lyophilized AST-NLC.The characteristics of AST-NLC,including shape,size,PDI,Zeta potential,entrapment efficiency(EE%) and drug loading(DL%),before and after freeze-drying were investigated.RESULTS Satisfied lyophilized AST-NLC could be prepared using 10% sucrose as the supporting agent.The freeze-drying process was as follow:pre-cooled at 40 ℃ for 4 h,freeze-drying for 24 h.AST-NLC presented a spherical shape under transmission elecctron microscopy(TEM).The characteristics before freeze-drying were as follows:average diameter was 104.3±1.25 nm,PDI was 0.118±0.033,Zeta potential was-7.00±0.35 mV,entrapment efficiency and drug loading were 94.37%±0.39% and 2.80%±0.02%,respectively.After freeze drying,the average diameter was 144.1±17.08 nm,PDI was 0.132±0.055,Zeta potential was-11.2±0.9 mV,the entrapment efficiency and drug loading were 96.60%±0.45% and 2.60%±0.05%,respectively.CONCLUSION The preparation of AST-NLC is convenient and the produced AST-NLC has a high entrapment efficiency.Satisfied lyophilized AST-NLC can be prepared using 10% sucrose as the supporting agent.
出处
《华西药学杂志》
CAS
CSCD
北大核心
2011年第6期530-533,共4页
West China Journal of Pharmaceutical Sciences
关键词
黄芪甲苷
纳米结构脂质载体
包封率
冷冻干燥
Astragaloside IV
Nanostructured lipid carriers
Entrapment efficiency
Freeze-drying