莪术油纳米脂质载体给药系统的制备及其评价

 目的研制莪术油纳米脂质载体系统。方法采用熔融超声-低温固化法制备莪术油纳米质脂载体系统,考察载药纳米粒的形态、粒径、Zeta电位等理化性质;用HPLC测定药物的包封率及体外释放特性;采用肝内隧道植入法,在小鼠H-22移植瘤模型上观察两种莪术油制剂的体内抑瘤活性。结果制得的纳米粒在透射电镜下均呈圆球形,平均粒径为(82.26±3.63)nm,Zeta电位为-(23.53±1.29)mV,制剂中吉玛酮的质量浓度为(0.972±0.021)g·L^-1,包封率为(94.95±1.87)%。结论熔融超声-低温固化法应用于莪术油等挥发油类药物纳米分散给药系统的制备是可行的,对小鼠体内H-22肉瘤株有显著的抑制效果。

Preparation and Evaluation of Zedoary Turmeric Oil Nanostructuded Lipid Carriers Delivery Systems

OBJECTIVE To investigate the preparation of zedoary turmeric oil nanostructured lipid carriers(ZTO-NLC).METHODS ZTO-NLC were prepared using the hot dispersion-cool solidification method. The morphology, mean diameter (MD) and Zeta potential of ZTO-NLC were used to evaluate the influence of different formulation and preparation factors;the contents of dispersion and entrapment efficiency of ZTO-NLC were determined by HPLC.Orthotopic transplation tumor model of hepatoma in mice were used to observe the inhibitory effects of zedoary turmeric oil on H-22 cells in vivo.RESULTS The ZTO-NLC in electron microscopy were spherical in shape, the mean diameter of ZTO-NLC was (82.26±3.63)nm, Zeta potential was -(23.53±1.29)mV,the content of Germacrone was (0.972±0.021)g·L^-1,the encapsulation efficiency of Germacrone was (94.95±1.87)%, and the microspheres were in good shape. CONCLUSION It is able to prepare nano-delivery system with volatiable oil,such as zedoary turmeric oil,by hot dispersion-cool solidification method. ZTO-NLC has marked inhibitory effects on mice H-22 cells in vivo.