混合组分挥发油纳米乳的处方筛选与体外透皮性能研究  

Formulation Screening and in vitro Transdermal Behavior of Nanoemulsions Loaded with Mixed Volatile Oils

作　　者：管咏梅 胡育森 刘佳 孔招娣 陈丽华 GUAN Yongmei;HU Yusen;LIU Jia;KONG Zhaodi;CHEN Lihua(Key Lab.of Modern Preparation of TCM,Ministry of Education,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004)

机构地区：[1]江西中医药大学现代中药制剂教育部重点实验室,江西南昌330004

出　　处：《中国医药工业杂志》2020年第11期1410-1410,1411-1417,共8页Chinese Journal of Pharmaceuticals

基　　金：江西省教育厅科学研究基金(GJJ170705);江西省重大科技研发专项(20194ABC28009)。

摘　　要：采用最大容水量法、电导率-含水量曲线法及伪三元相图法,初步筛选出空白纳米乳的处方组成;再以平均粒径和多分散系数(PDI)为评价指标,采用Box-Behnken设计-响应面法进行优化,确定空白纳米乳的优化处方为:混合表面活性剂(Tween-80∶聚乙二醇-40氢化蓖麻油=1∶4)∶助表面活性剂(无水乙醇)∶油相(单辛酸甘油酯)=22∶11∶8。将五味子、石菖蒲、郁金、香附按解郁安神方的比例(1∶1∶1∶1)混合,采用水蒸气蒸馏法提取得到混合挥发油。向优化空白纳米乳中加入3%混合挥发油,所得纳米乳的电导率为(141.10±1.53)μS/cm,粒径为(20.97±0.18)nm,PDI为0.143±0.010;并且在25℃贮存30 d,粒径和PDI无明显变化。体外透皮试验结果显示,纳米乳中混合挥发油的指标成分甲基丁香酚、榄香素、β-细辛醚、α-细辛醚的24 h累积透过量分别为(417.48±8.63)、(501.83±14.02)、(405.40±13.41)和(48.37±0.91)μg/cm^2,在8 h内4个指标成分的释放数据均符合Higuchi方程。Firstly,the formulation of blank nanoemulsions was selected according to the determination of maximum water holding capacity,conductivity-water content curves and pseudo-ternary phase diagrams.Then,the Box-Behnken design-response surface methodology with average particle size and polydispersity index(PDI)as evaluation indexes was adopted to further optimize.The optimal formulation of blank nanoemulsions was composed of compound?surfactants(Tween-80∶PEG-40 hydrogenated castor oil=1∶4),cosurfactant(anhydrous ethanol)and oil phase(glycerol?monocaprylate)in the ratio of 22∶11∶8.The mixed volatile oils were extracted by steam distillation from the mixture of Schisandra chinensis,Acorus tatarinowii,Radix Curcumae and Cyperus rotundus in a mass ratio of 1∶1∶1∶1,which were the crude drugs used in Jieyu Anshen formula.Then,3%of mixed volatile oils were added into above optimized blank nanoemulsions,and the title nanoemulsions were obtained with conductivity of(141.10±1.53)μS/cm,average particle size of(20.97±0.18)nm,and PDI of 0.143±0.010.In addition,the particle size and PDI did not change significantly during storage at 25℃for 30 d.The results of transdermal test in vitro showed that the cumulative permeation amount at 24 h for four index components,namely methyl eugenol,elemicin,β-asarone?and?α-asarone,from the nanoemulsions were(417.48±8.63),(501.83±14.02),(405.40±13.41),and(48.37±0.91)μg/cm^2,respectively.The release data within 8 h of four index components were in accordance with Higuchi equation.

关 键 词：挥发油 纳米乳 电导率 伪三元相图法 Box-Behnken设计-响应面法 

分 类 号：R944.9[医药卫生—药剂学]