辣蓼黄酮长循环纳米脂质体的制备

Preparation of Polygonum hydropiper flavone long circulating nano liposomes

研究旨在优化辣蓼黄酮长循环纳米脂质体制备条件。试验首先以包封率为评价指标,筛选辣蓼黄酮长循环纳米脂质体制备方法。确定改良乙醇注入法后,采用单因素试验考察磷胆比、药脂比、生理盐水体积、超声时间、表面活性剂用量因素对包封率的影响;再通过Box-Behnken响应面法进行3因素3水平优化,选取磷胆比、药脂比、生理盐水体积等3个因素进一步优化;确定最佳的脂质体制备条件后,通过后插入法将DSPEMPEG 2000插入辣蓼黄酮纳米脂质体上,制成辣蓼黄酮长循环纳米脂质体并进行表征。结果显示,改良乙醇注入法制备辣蓼黄酮长循环纳米脂质体最优条件是:磷胆比(质量比)6.8∶1、药脂比(质量比)1∶10.3、生理盐水体积9.5 mL。选择摩尔比为5%的DSPE-MPEG 2000制备长循环纳米脂质体,在最优条件下制备的辣蓼黄酮长循环纳米脂质体平均包封率为(72.60±2.44)%,脂质体粒径为(80.93±0.30)nm,多分散性指数(PDI)为0.14±0.01,Zeta电位(-1.70±0.29)mV。

The aim of the study was to optimize the preparation conditions of Polygonum spicicum flavone long cycle nano liposome.The encapsulation rate was taken as the evaluation index to compare the modified ethanol injection method,film dispersion method,reverse evaporation method and ordinary ethanol injection method.After the modified ethanol injection method was determined,the factors of phosphorus-bile ratio,drug-lipid ratio,normal saline volume,ultrasonic time and surfactant dosage were investigated by single factor test.Then Box-Behnken response surface method was used to optimize three factors and three levels,and phosphorus bile ratio,drug lipid ratio and normal saline volume were selected.After determining the best preparation conditions of Polygonum spicum L.flavone nano-liposomes,DSPE-MPEG 2000 was inserted into Polygonum spicum L.flavone nano-liposomes by post-insertion method to prepare Polygonum spicum L.flavone long-cycle nano-liposomes and characterize them.The results showed that the optimal conditions for preparation of Polygonum spicum flavone long-cycle nano liposomes by modified ethanol injection method were as follows phosphorus bile ratio(mass ratio)6.8:1,drug lipid ratio(mass ratio)1:10.3 and normal saline volume 9.5 mL.The average encapsulation rate,particle size and polydispersity index of polygonum spicum flavonoids were(72.60±2.44)%,(80.93±0.30)nm and(0.14±0.01)respectively prepared by DSPE-MPEG 2000 with a molar ratio of 5%.Zeta potential(-1.70±0.29)mV.