芹菜素囊泡的制备及理化性质考察

Preparation of apigenin niosomes and properties investigation

目的筛选合适的非离子表面活性剂,制备芹菜素囊泡,并考察其体外理化性质和冻干工艺。方法采用Tween80和Myrij52为成囊材料,建立了乙醇注入法制备芹菜素囊泡的制备工艺;采用微柱离心法测定芹菜素囊泡的包封率,并考察不同处方因素对包封率的影响;经正交设计得到最优处方;对囊泡的粒径、外观、稳定性等理化性质及体外释放行为进行研究,分别以外观、粒径和渗漏率为指标对冻干工艺进行初步考察。结果乙醇注入法获得囊泡包封率为(69.48±2.5)%,平均粒径为(148±5.03)nm,透射电镜下观察显示呈类球形,4℃下密封保存3个月包封率为(54.25±3.7)%、渗漏率为21.9%,在pH值为7.4的磷酸盐缓冲液中体外释药行为符合一级动力学方程。以葡萄糖和甘露醇(质量比1∶1)为冻干保护剂,预冻时间为3 h,干燥时间为30 h。结论该制剂制备方法简单,制备的囊泡包封率较高,粒径较小,体外具有明显的缓释作用,冻干制剂外观饱满,粒径和包封率变化较小,可以明显提高囊泡的体外稳定性。

Objective To prepare the apigenin niosomes and freeze-dried apigenin niosomes with suitable nonionic surfactant and investigate the physico-chemical properties of the niosomes. Methods Apigenin nio- somes were prepared with Tween 80 and Myrij 52 by ethanol injection method, and the entrapment efficiency was determined with microcolumn centrifugalization. The formulation was optimized by orthogonal design and physico-chernieal property of the niosome was also investigated, the appearance of niosome was observed by transmission electron microscope and their particle size was determined by laser light scattering technique. The lyophilization process was studied, the various influence on the appearance, particle size and the leakage rate of the lyophilization product was investigated. Results The entrapment efficiency of the niosomes was（ 69. 48 ±2. 5）%, the average particle size was （148 ±5.03 ）nm, and the shape of apigenin nio- somes was spherical. The entrapment efficiency at 4 ℃ after 3 months was （54. 25± 3.7 ） % and the leakage rate of apigenin from niosomes was 21.9 %. The release followed the fast order kinetic equation. The protectants were glucose and mannitol（m： m = 1： 1） ,the time of freezing was 3 h,the time used in drying was 30 h. Conclusions Apigenin niosomes can prolong the drug release time in vitro. The preparation process of apigenin niosomes is simple with higher entrapment efficiency and smaller particle size. The appearance after lyophilization is satiation, there is little change in particle size and entrapment efficiency, the stability of the niosomes is significantly elevated by freeze-drying.