两种鬼臼毒素脂质体的制备及其比较分析

Preparation and comparative analysis of two podophyllotoxin liposomes

目的制备两种含有鬼臼毒素(PPT)的脂质体凝胶剂并比较两者的性能.方法采用逆向蒸发法制备PPT-二棕榈酰磷脂酰胆碱(DPPC)和PPT-大豆卵磷脂脂质体,光镜和电镜观察2种脂质体的外观形态并测定粒径大小.采用凝胶渗透色层技术测定脂质体的包封率.结果 PPT-DPPC脂质体光镜下为球形,粒径为0.825～2.050 μm,平均1.450 μm;PPT-大豆卵磷脂脂质体粒径1.445～7.590μm,平均3.780μm.电镜下PPT-DPPC脂质体的结构为多室脂质体,包封率为73.8%;PPT-大豆卵磷脂脂质体包封率为79.1%.室温保存1个月后测得PPT-DPPC脂质体的包封率为65.2%、3个月为58.8%,6个月后为56.4%;PPT大豆卵磷脂脂质体的包封率则依次为70.3%、60.4%和51.3%.结论使用逆向蒸发法制备鬼臼毒素的脂质体凝胶剂,方法简便易行,分布较均匀,包封率较高.

Objective To prepare two different liposome gels containing podophyllotoxin (PPT) and compare their pharma-ceutical properties. Methods PPT-Dipalmitoylphosphatidylcholine (DPPC) liposome and PPT-soya lecithin liposome were prepared by reverse phase evaporation technique, and optical and electron microscopy were performed respectively for exam-ining the appearances of the 2 liposomes and the diameter of the particles. Gel filtration was employed to assess the embed-ding ratio of the liposomes. Results Under optical microscope, PPT-DPPC liposome was observed to be composed of spheri-cal particles with diameter range of 2.05~0.825 μm (average 1.45 μm). The diameter range of the particles of PPT-soya lecithin liposome is 7.59~1.445 μm (average 3.78 μm) . PPT-DPPC liposome appeared multivesicular under electron micro-scope, with the embedding ratio of 73.8%, and 79.1% for PPT-soya lecithin liposome (n=3). PPT-DPPC liposome had a em-bedding ratio of 65.2%, 58.8% and 56.4% after preserved 1, 3, 6 months respectively. As for PPT-soya lecithin liposome, the embedding ratios were 70.3%, 60.4%, and 51.3% respectively. Conclusion The PPT in the liposomes prepared by reverse phase evaporation technique is evenly distributed throughout the gel. The preparation is relatively simple with high embedding ratio.