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两种鬼臼毒素脂质体的制备及对比分析

Preparation and comparative analysis of two podophyllotoxin liposomes.

作者信息

Hou Gui-rong, Zeng Kang, Zhou Zai-gao, Li Guo-feng

机构信息

Department of Dermatology, Nanfang Hospital, First Military Medical University, Guangzhou 510515, China.

出版信息

Di Yi Jun Yi Da Xue Xue Bao. 2003 Mar;23(3):216-8.

Abstract

OBJECTIVE

To prepare two different liposome gels containing podophyllotoxin (PPT) and compare their pharmaceutical 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 examining the appearances of the 2 liposomes and the diameter of the particles. Gel filtration was employed to assess the embedding ratio of the liposomes.

RESULTS

Under optical microscope, PPT-DPPC liposome was observed to be composed of spherical particles with diameter range of 2.05 to 0.825 microm (average 1.45 microm). The diameter range of the particles of PPT-soya lecithin liposome is 7.59 to 1.445 microm (average 3.78 microm). PPT-DPPC liposome appeared multivesicular under electron microscope, with the embedding ratio of 73.8%, and 79.1% for PPT-soya lecithin liposome (n=3). PPT-DPPC liposome had a embedding 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.

摘要

目的

制备两种含鬼臼毒素(PPT)的不同脂质体凝胶,并比较它们的药学性质。

方法

采用逆相蒸发技术制备PPT-二棕榈酰磷脂酰胆碱(DPPC)脂质体和PPT-大豆卵磷脂脂质体,分别用光学显微镜和电子显微镜观察两种脂质体的外观及颗粒直径。采用凝胶过滤法评估脂质体的包封率。

结果

光学显微镜下,观察到PPT-DPPC脂质体由直径范围为2.05至0.825微米(平均1.45微米)的球形颗粒组成。PPT-大豆卵磷脂脂质体颗粒的直径范围为7.59至1.445微米(平均3.78微米)。电子显微镜下,PPT-DPPC脂质体呈多囊泡状,包封率为73.8%,PPT-大豆卵磷脂脂质体的包封率为79.1%(n = 3)。PPT-DPPC脂质体在保存1、3、6个月后的包封率分别为65.2%、58.8%和56.4%。对于PPT-大豆卵磷脂脂质体,包封率分别为70.3%、60.4%和51.3%。

结论

采用逆相蒸发技术制备的脂质体中的PPT均匀分布于整个凝胶中。该制剂制备相对简单,包封率高。

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