摘要
目的优化筛选葛根素纳米脂质体(puerarin nano-liposomes carriers,Pue-NLC)的制备工艺,并考察其体外释放特性。方法采用高压均质法制备Pue-NLC,正交设计优化筛选处方,HPLC法测定含量,超高速离心法结合甲醇提取法测定包封率和载药量,透射电镜观察外观,激光粒度测定仪测定其平均粒径和Zeta电位,透析袋法考察体外释放特性。结果最优工艺处方为葛根素(Pue)50 mg,2.0%单硬脂酸甘油酯(GP)∶辛酸葵酸三甘油酯(LLW)为200∶160(W/W),0.5%泊洛沙姆(F68)水溶液,制备的Pue-NLC外观呈圆形或椭圆形,平均粒径为(102.4±5.6)nm,多分散系数为0.214±0.027,Zeta电位为(-18.8±2.7)mV,包封率为(45.9±1.43)%,载药量为(0.81±0.05)%,在生理盐水中的体外释药行为符合Weibull方程:In[In(1/1-Q)]=1.143 3 Int-0.547 0,r=0.986 0,24 h释放率为88.15%。结论高压均质法成功制备了Pue-NLC,粒径小,载药量和包封率高,具有缓释特性,具有一定的开发前景,为葛根素新型给药系统的研究提供理论基础和实践指导。
Objective To investigate the optimal preparation and prepare of Puerarin Nano-liposomes Car- r iers,and to evaluate its in vitro release property. Methods Using high pressure homogenization to prepare puerarin nano-liposomes,optimizing and screening the prescription by orthogonal design optimization,HPLC to determinate the content of Puerarin,ultra-high speed centrifugal combination with methanol extraction to determinate the encapsulation efficiency and drug loadings rate,transmission electron microscope to observe appearance,laser particle size tester to determine the average particle size and Zeta potential,dialysis bag method to investigate in vitro release characteristics. Results The results showed that Pue-NLC were uniform size and round,and formed of（102.4 ±5.6） nmin particle size with PDI of 0.214 ±0.027,Zeta potential of（-18.8 ±2.7） mV,entrapment efficiency of（ 45. 9 ± 1. 43） %,and drug loading of（ 0. 81 ± 0. 05） %. The in vitro release profiles in saline conform to the Weibull equation： ln[ln（ 1 /1- Q） ]= 1. 143 3 lnt- 0. 547 0,r = 0. 986 0,and 24 h release rate was88. 15%. Conclusion High pressure homogenization prepared Pue-NLC successfully,with small particle size,high drug loadings rate and encapsulation efficiency,and slow-release characteristics. Pue-NLC has a certain development prospects,will provide theoretical basis and practical guidance for research of puerarin new drug delivery system.
出处
《甘肃中医学院学报》
2014年第3期41-46,共6页
Journal of Gansu College of Traditional Chinese Medicine
关键词
葛根素
纳米脂质体
高压均质法
正交设计
体外释放
Puerarin
Nano-liposomes Carriers
high pressure homogenization
orthogonal design
in vitro release
