载高乌甲素橄榄油微乳的制备及其性能研究

Preparation of Lappaconitine-Loaded Microemulsion with Olive Oil and Research on Its Properties

目的制备载高乌甲素(LA)橄榄油微乳,并研究其形态、粒径、载药量、释药行为及流变学特性。方法采用伪三相图法进行载LA橄榄油微乳的处方筛选与制备,动态透析法考察其体外释药性能,运用MCR 301流变仪研究其流变学性能。结果载LA橄榄油微乳的最优处方为:橄榄油为油相,蓖麻油聚氧乙烯醚-40/司盘-80(4∶1)为表面活性剂,丙三醇为助表面活性剂,Km=3。微乳的形态呈圆形或椭圆形,平均粒径(91±0. 55) nm,载药量1. 85%。体外释药实验表明,微乳对于LA的释放具有一定的缓释作用,其释药行为可用Higuchi方程描述。流变学研究表明,载LA橄榄油微乳属于非牛顿流体中的假塑性流体,具有剪切稀化的性质,属于触变体系,有一定的黏弹性。结论成功制备了载LA橄榄油微乳,且微乳具有一定的缓慢释药行为和较好的流变学性质,本实验为载LA橄榄油微乳的制剂开发奠定了基础。

OBJECTIVE To prepare lappaconitine( LA)-loaded microemulsion with olive oil and study its morphology,particle size,drug loading capacity,drug release behavior and rheological characteristics. METHODS Pseudo-ternary phase diagram method was used to screen and prepare LA-loaded microemulsion with olive oil. LA release properties in vitro were investigated by dynamic dialysis method. The rheological properties of LA-loaded microemulsion with olive oil were studied using MCR 301 rheometer. RESULTS The optimal formulation of LA-loaded microemulsion with olive oil was as follows: olive oil was the oil phase,castor oil polyoxyethylene ether-40/span-80( 4∶ 1) was the surfactant,glycerin was the cosurfactant,and Km= 3. The morphology of the microemulsion particles was round or oval,and the average particle size was( 91 ± 0. 55) nm. The drug-loading rate of LA in the microemulsion was 1. 85%. Drug release experiments in vitro showed that the microemulsion had a sustained release effect on LA,and the drug release behavior was more suitable to be described by Higuchi equation. Rheological experiments showed that the fluid of LA-loaded microemulsion with olive oil belong to pseudoplastic fluid of non-Newtonian fluid exhibiting thixotropic and shear-thinning fluid behavior as well as certain viscoelasticity. CONCLUSION The LA-loaded microemulsion witholive oil are successfully prepared,and the microemulsion has ideal sustained release behavior and good rheological properties. The study provides a foundation for the developmenton preparation of LA-loaded microemulsion with olive oil.