0.5%鬼臼毒素纳米脂质载体的制备及理化性质考察

Preparation and Evaluation of 0.5% Podophyllotoxin-Loaded Nanostructured Lipid Carrier

目的:纳米脂质载体(nanostructured lipid carrier,NLC)具有较高的载药量和物理稳定性。为提高鬼臼毒素(podophyllotoxin,POD)的治疗效果,降低毒副作用,本研究探讨了POD浓度为5 g/L(0.5%)的POD-NLC的制备方法及理化性质。方法:POD-NLC的制备采用乳化蒸发-低温固化法,设计正交实验优化POD-NLC的制备工艺及配方,用透射电镜、粒径仪、高效液相色谱法、pH计考察POD-NLC理化性质。结果:POD-NLC基本呈球状或椭球形,平均粒径(180±20)nm,多分散指数为0.165,pH值为6.20±0.04,包封率为(82.9±2)%。结论:成功制得了POD浓度为5 g/L(0.5%)的POD-NLC,其制备工艺简单,粒径分布较均匀,包封率高,稳定性较好。

Objective：Nanostructured lipid carrier（NLC） has high capacity of drug-loading and high physical stability.The aims of this paper are to investigate preparation method and physicochemical properties of podophyllotoxin-loaded NLC（POD-NLC） containing 5 g/L（0.5%） POD,and to improve therapeutic effect,as well as to reduce toxicity of podophyllotoxin（POD）. Methods：The POD-NLC was prepared with method of emulsion evaporation and subsequent solidification at a low temperature.The preparation conditions and prescription were optimized by an experiment designed with orthogonal method.The physicochemical properties of the POD-NLC were measured with transmission electronic microscope,particle size analyzer,high-performance liquid chromatography and pH meter,respectively. Results：The POD-NLC appeared as sphere or ellipsoid,with mean particle size of（180±20） nm,polydispersity index of 0.165 and pH value of 6.20±0.04.The entrapment efficiency of POD in the nanoparticles was（82.9±2）%. Conclusion：We have successfully prepared stable POD-NLC containing 5g/L（0.5%） POD with even distribution,good stability,high efficiency of encapsulation,and the simple preparation method.