姜黄素纳米脂质载体的制备、优化及体外评价  

Preparation,optimization and in vitro evaluation of curcumin-loaded nanostructured lipid carriers

作　　者：康玉霞[1,2] 雷丸 王济 王晓娟 

机构地区：[1]陕西中医药大学,陕西咸阳712046 [2]军事口腔医学国家重点实验室,第四军医大学口腔医院药剂科,陕西西安710032

出　　处：《中成药》2016年第5期1011-1017,共7页Chinese Traditional Patent Medicine

基　　金：陕西省中医药管理局中医药科研课题(15-ZY021)

摘　　要：目的制备、优化姜黄素纳米脂质载体,并进行体外评价。方法薄膜分散法制备姜黄素纳米脂质载体后,以粒径和包封率为评价指标,单因素和正交设计法优化处方和制备工艺。透射电镜观察其外观形态,激光粒度分析仪测定其粒径、粒径分布及Zeta电位,透析法测定其体外释放行为。结果最优条件为投药量10 mg,固液比2∶5,超声时间6 min,磷酸缓冲溶液p H值6.5。不同磷脂酰丝氨酸比例(0%、4%、8%、12%)修饰的载体呈球形或类球形,分布均匀,平均粒径分别为(212.1±1.4)、(210.5±1.3)、(207.6±1.7)、(198.4±1.7)nm,Zeta电位分别为(-1.33±0.39)、(-18.01±0.41)、(-45.31±0.36)、(-45.56±0.41)m V,包封率分别为(85.64±0.67)%、(86.13±0.56)%、(88.38±0.34)%、(88.78±0.58)%,载药量分别为(2.23±0.03)%、(2.15±0.03)%、(2.19±0.04)%、(2.18±0.02)%,具有明显的缓释特性。结论制备的姜黄素纳米脂质载体粒径分布均匀,包封率和载药量均良好。AIM To prepare and optimize curcumin-loaded nanostructured lipid carriers and to evaluate in vitro performance. METHODS For curcumin-loaded nanostructured lipid carriers prepared by film dispersion method,single factor test and orthogonal design method were applied to optimizing its formulation and preparation technology,with regard to indices of particle size and encapsulation efficiency. The morphology was studied by transmission electron microscopy,while the particle size,particle distribution and Zeta potential were determined by laser particle size analyzer,and the in vitro drug release behavior was investigated by dialysis method. RESULTS The following conditions were 10 mg for dosage,2 ∶ 5 for ratio of solid to liquid,6 min for extraction time and 6. 5 for p H value of phosphate buffer solution. The carriers modified by different ratios of phosphatidylserine（ 0%,4%,8% and 12%） were spherical or approximately spherical with homogeneous distribution. The mean sizes were（ 212. 1 ± 1. 4） nm,（ 210. 5 ± 1. 3） nm,（ 207. 6 ± 1. 7） nmand（ 198. 4 ± 1. 7） nm,the Zeta potentials were（-1. 33 ± 0. 39） m V,（-18. 01 ± 0. 41） m V,（-45. 31 ± 0. 36） m Vand（-45. 56 ± 0. 41） m V,the encapsulation efficiencies were（ 85. 64 ± 0. 67） %,（ 86. 13 ± 0. 56） %,（ 88. 38 ± 0. 34） % and（ 88. 78 ±0. 58） %,and the drug loading capacities were（ 2. 23 ± 0. 03） %,（ 2. 15 ± 0. 03） %,（ 2. 19 ± 0. 04） % and（ 2. 18 ± 0. 02） %,respectively. An obvious slow-release character was observed. CONCLUSION The obtained curcumin-loaded nanostructured lipid carriers display a uniform particle size distribution with high encapsulation efficiency and drug loading capacity.

关 键 词：姜黄素纳米脂质载体 制备 优化 体外评价 薄膜分散法 单因素 正交设计 

分 类 号：R944[医药卫生—药剂学]