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目的:制备了以氢化大豆磷脂(HSPC)和普通大豆磷脂(SPC)为膜材的马钱子总生物碱复合磷脂脂质体,并与相应的单一磷脂脂质体比较药剂学性质。方法:采用浸渍法提取马钱子总生物碱并进行了纯化。采用硫酸铵梯度法和隐形脂质体技术制备了马钱子总生物碱复合磷脂脂质体和相应的2种单一磷脂(HSPC,SPC)脂质体,比较了3者的包封率、粒径、电位、释放度等性质。结果:HSPC-SPC(1∶3)为载药效果最好的复合磷脂比例。当药脂质量比为1∶6时,马钱子总生物碱复合磷脂、SPC和HSPC脂质体的包封率分别为(73.6±2.9)%,(62.9±1.8)%和(54.7±1.0)%(n=3)。与2种单一磷脂脂质体相比,马钱子总生物碱复合磷脂脂质体粒径明显减小但电位没有差别。释放度显著提高,但加入大鼠血浆后,复合磷脂脂质体的释放度显著低于SPC脂质体。结论:考虑到包封率提高、血液中稳定以及磷脂的价格,作为中药抗肿瘤药物载体,复合磷脂脂质体比相应的单一磷脂脂质体更具有开发价值。
OBJECTIVE: The total alkaloids of Strychnos cholerae combined with hydrogenated soya phospholipid (HSPC) and common soya lecithin (SPC) were prepared and their pharmacological properties were compared with that of single phospholipid liposomes. Methods: The total alkaloids of Strychnos nux - vomica were extracted and purified by dipping method. Strychnos alkaloids complex phospholipid liposomes and two kinds of single liposome (HSPC, SPC) liposomes were prepared by ammonium sulfate gradient method and invisible liposome technique. The encapsulation efficiency, Diameter, potential, release and other properties. Results: HSPC-SPC (1: 3) was the best proportion of compound phospholipids. The entrapment efficiency of total Strychnos alkaloids complex phospholipids, SPC and HSPC liposomes were (73.6 ± 2.9)%, (62.9 ± 1.8)% and (54.7 ± 1.0) )% (n = 3). Compared with the two kinds of single phospholipid liposomes, Strychnos alkaloids complex phospholipid liposome size was significantly reduced but no difference in potential. Release significantly increased, but the addition of rat plasma, the release of complex phospholipid liposomes was significantly lower than the SPC liposomes. Conclusion: Considering the increase of entrapment efficiency, blood stability and the price of phospholipids, as a traditional Chinese medicine anticancer drug carrier, the complex phospholipid liposomes have more developmental value than the corresponding single phospholipid liposomes.