苦参总碱纳米乳的理化性质及其体外透皮实验研究

Physicochemical properties and skin penetration in vitro of total alkaloids of Sophora flavescens nanoemulsion

该实验主要考察苦参总碱纳米乳的理化性质、稳定性及体外透皮特性。制备苦参总碱纳米乳,采用HPLC测定纳米乳中苦参碱和氧化苦参碱的含量,分别采用透射电镜和激光粒度仪观察纳米乳的形态和测定粒径,并对苦参总碱纳米乳在低温(4℃)、常温(25℃)以及高温(60℃)条件下的稳定性进行考察。最后采用Franz扩散池对纳米乳的体外透皮特性进行研究。结果发现该实验制备的苦参总碱纳米乳外观圆整、均匀,平均粒径为(15.55±2.24)nm,粒径分布值0.161;在4,25,60℃条件下放置15 d,其外观、粒径及含量未发生明显变化;苦参总碱纳米乳的稳态渗透速率J为4.564 1μg·cm-2·h-1;24h的累积渗透量为110.7μg·cm-2,是水溶液24 h累积渗透量(59.41μg·cm-2)的1.86倍。实验表明苦参总碱纳米乳具有良好的透皮效果,可为其临床应用提供一种新剂型。

The research aimed at investigating the physicochemical properties, stability and skin penetration in vitro of total al- kaloids of Sophora flavescens nanoemulsion. Prepare total alkaloids of S. flavescens nanoemulsion and detect the determination of ma- trine and oxymatrine in the nanoemulsion using HPLC method. Transmission electron microscopy and laser particle size analyzer were utilized to detect the shape and size of the nanoemulsion respectively. And also the stability of nanoemulsion was studied under the con- ditions of low temperature （4 ℃ ）, normal temperature （25 ℃ ） and high temperature （60 ℃ ）. Franz diffusion cell was used to re- search the transdermal absorption of nanoemulsion in vitro. The results found that the nanoemulsion we prepared presented appearance of rounded, uniform; its average diameter was （ 15.55± 2.24） nm, and particle size distribution value was 0. 161 ; the appearance, diameter and percentage determination of total alkaloids of S. flavescens had no variations after 15 d under 4, 25, 60 ℃ respectively. The steady-state permeation rate was 4. 564 1 μg·cm^-2 ·h-1, 24 h cumulative amount of penetration was 110.7 μg·cm^-2 , which was 1.86 fold of 24 h cumulative amount of aqueous solution（59.41 μg·cm^-2）. All the results demonstrated total alkaloids of S. fla- vescens nanoemulsion had good permeability, and could provide a new preparation for its clinical application.