星点设计-效应面法优化载人参多成分纳米脂质载体处方研究  

Optimization of Preparation of Nanostructured Lipid Carriers Loaded with Ingredients of Ginseng by Central Composite Design-Response Surface Methodology

作　　者：尚尔雨 马晓乾 孙爽[2] 申国涛 Shang Eryu;Ma Xiaoqian;Sun Shuang;Shen Guotao(Heilongjiang Forest Protection Institute, Harbin 150040, China;Heilongjiang University of Chinese Medicine, Harbin 150040, China)

机构地区：[1]黑龙江省森林保护研究所,哈尔滨150040 [2]黑龙江中医药大学,哈尔滨150040

出　　处：《黑龙江科学》2022年第14期1-6,11,共7页Heilongjiang Science

摘　　要：采用星点设计-效应面法,优化载人参多成分齐墩果酸(Oleanolic Acid)、熊果酸(Ursolic Acid)、人参皂苷Rg3(Ginsenosider Rg3)纳米脂质载体(OUR-NLC)的处方。采用正交设计对载中药多成分纳米脂质载体处方主要影响因素进行初步筛选,设计独立因素:药物用量比为X1,表面活性剂浓为X2,油酸用量为X3、X4,建立二水平表,将Y1(总包封率,%)、Y2(总载药量,%)设计为响应参数,依据星点设计法进行试验。对结果采用二项式方程拟合,经效应面法预测最佳处方。优化处方制备中药多成分纳米脂质载体,优化后的处方为:水和油的体积比为1.9∶1(mL/mL),药物量14.5 mg,C乳化剂为0.1%。根据优化处方所制备的OUR-NLC的包封率为(44.35±1.46)%,载药量(8.99±0.10)%,平均粒径为(99.04±2.09)nm,多分散指数(PDI)为0.227±0.001,Zeta电位为(72.00±1.25)mV。采用星点设计-效应面法优化处方,实测值与预测值偏差率较小,各项指标的偏差均小于±5%,星点设计-效应面法的预测效果及稳定性良好,包封率高,方法可靠。The study adopts central composite design-response surface methodology,and optimizes the prescription of OUR-NLC,which include Oleanolic Acid,Ursolic Acid and Ginsenosider Rg3.Firstly,the main factors of preparation of nanostructured lipid carriers loaded with multicomponent of TCM is preliminary screened by using orthogonal design.Then,we design the second level table by taking drug dosage ratio,surfactant concentration,dosage of oleic acid as independent factors X1,X2,X3 and X4 respectively,and using total entrapment efficiency(Y1,%),total drug loading(Y2,%)as response parameters.The optimal formulation of making nanostructured lipid carriers loaded with multicomponent of TCM is as follows:water oil volume ratio is 1.9∶1(mL/mL),drug dosage is 14.5mg,and emulsifier concentration is 0.1%.Entrapment efficiency of OUR-NLC which is made according to the optimal prescription is(44.35±1.46)%,drug loading is(8.99±0.10)%,average particle size is(99.04±2.09)nm,PDI is(0.227±0.001),and Zeta potential is(72.00±1.25)mV.The prescriptions are optimized by central composite design-response surface methodology.The deviation between the measured values and predicted values is small.Each index deviation is less than±5%.The prediction central composite design-response surface methodology is a reliable method which has a good stability and high entrapment efficiency.

关 键 词：中药多成分 纳米脂质载体 星点设计-效应面法 包封率 载药量 

分 类 号：R283.6[医药卫生—中药学]