鬼臼毒素纳米脂质载体的制备及质量考察

目的：纳米脂质载体是近年来继固体脂质纳米粒发展起来的第2代亚微粒载药系统，具有较高的载药量和物理稳定性。探讨鬼臼毒素-脂质纳米粒（podophyllotoxin-loaded nanostructured lipid carrier，PPT-NLC）的制备方法及理化性质。方法：实验于2006—08／2007—10在南方医科大学药学部实验室完成。选择固体脂质硬脂酸、单硬脂酸甘油脂和液态脂质油酸，采用改良的乳化蒸发-低温固化法制备PPT-NLC，用同法制备不含油酸的PPT-固体脂质纳米粒（Solid lipid nanoparticles，SLN）纳米粒混悬液。用透射电镜、Zeta电位仪、高效液相色谱法、pH计考察PPT—NLC理化性质，并比较SLN与NLC的包封率和稳定性。结果：透射电镜下PPT—NLC外形呈圆形或椭圆形，平均粒径为（88．2±8.4）nm，多分散指数为0．190±0．085，Zeta电位为（-33．2±3．1）mV，包封率为86．6％。PPT-SLN分别为（75．3±16．2）nm，0．300±0．072，（-25．2±3．4）mV，包封率为76．5％。结论：PPT-NLC制备工艺简单，分布均匀，稳定性较SLN好，包封率高。

Preparation and characterization of podophyllotoxin-loaded nanostructured lipid carriers

AIM： Nanostructured lipid carriers （NLC） have been developed as the second generation nanoparticulate delivery system, and possess the advantages of higher drug loading and physical stability. This study is designed to investigate the preparation method and physicochemical properties of podophyllotoxin-loaded NLC （PPT-NLC）. METHODS： This experiment was carried out in the laboratory of Pharmacy Department, Nanfang Hospital, Southern Medical University between August 2006 and October 2007. PPT-NLC was prepared by the method of emulsion evaporation and solidification at a low temperature. Monostearin, stearic acid and oleic acid were all used as lipids. PPT-solid lipid nanoparticles （PPT-SLN） suspension without oleic acid was also prepared by means of the same method. The physicochemical properties of the PPT-NLC were investigated with transmission electronic microscope, Zeta potential analyzer, high-performance liquid chromatography and pH value, respectively. Then drug entrapment efficiency and physical stability were compared between NLC and SLN. RESULTS： Under transmission electronic microscope, PPT-NLC appeared as round or ellipse shape. The mean particle size, polydispersity index, Zeta potential and entrapment efficiency of PPT- NLC in the nanoparticles were （88.2 ± 8.4） nm, 0.190±0.085 （-33.2±3.1） mV and 86.6%, respectively. Likewise, these index of PPT-SLN were （75.3±16.2） nm, 0.300±0.072, （-25.2±3.4） mV and 76.5%, respectively. CONCLUSION： The PPT-NLC has simple preparation, even distribution, good stability and high efficiency of encapsulation compared with SLN.