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冻干保护剂和复水溶液对HB-Ⅰa脂质体包封率的影响

Effects of lyoprotectents and rehydrated solutions on the encapsulation of HB-Ⅰa liposomes

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【作者】 苏树强华泽钊丁志华胡水根韩林

【Author】 SU Shu-qiang, HUA Ze-zhao, DING Zhi-hua, HU Shui-gen, HAN Lin(Institute of Cryobiology and Food Engineering, Shanghai University of Science andTechnology, Shanghai 200093, China ;The Naval Pharmaceutical Science Center,411 Naval Hospital, Shanghai 200081, China)

【机构】 上海理工大学低温医学与食品工程研究所海军411医院药学专科中心海军411医院药学专科中心 上海 200093上海 200093上海 200434上海 200434

【摘要】 目的:研究不同保护剂种类与浓度、不同复水溶液对HB-Ⅰa脂质体冻干前后包封率的影响。方法:按不同配方进行了18组对比实验,通过比较各组脂质体冻干前后包封率,优选较好的HB-Ⅰa脂质体冻干工艺。结果:在对HB-Ⅰa脂质体包封率的提高与冻干保护方面,蔗糖及甘氨酸所组成的二元保护剂显示了较好的效果;在保护剂使用过程中,过高或过低的蔗糖浓度对提高冻干HB-Ⅰa脂质体的包封率不利;在复水溶液的使用方面,当保护剂蔗糖存在时,冻干后缓冲液复水较纯水复水包封率高。结论:以蔗糖-甘氨酸-卵磷脂-胆固醇-HB-Ⅰa(4:0.8:1:0.5:0.2)的配方配制的HB-Ⅰa脂质体包封率冻干前可达91.1%,冻干后可达85.6%。

【Abstract】 Objective: To study the effects of freeze-drying on the encapsulation of HB-Ⅰa lipo some with different kinds of lyoprotectents at various concentrations and different rehydrated solutions. Methods: Eighteen formulations of HB-Ⅰ a liposome were designed and their comparison studieswere performed. The optimized freeze-drying technique was selected based upon the encapsulation rate prior to and post freeze-drying. Results:The use of sucrose as a primary lyoprotectent and glycine as a supporting lyoprotectents provided a highest encapsulation rate and minimal change of HB-Ⅰa lipo somes. Sucrose at too high or too low concentrations failed to increase the encapsulation rate. At the presence of sucrose, the buffer solution showed a superior rehydration of freeze-dried HB-Ⅰa liposome to water. Conclusion: With an appropriate mass ratio of sucrose: glycine:phosphatidylcholine: cholesterol: HB-Ⅰ a( 4:0.8:1: 0.5: 0.2 ) the encapsulation rate of HB-Ⅰa liposome solution can be enhanced to 91.1% and 85.6% prior to and post the freeze-drying,respectively.

【基金】 国家自然科学基金重点项目(59836240);上海市教委重点学科建设项目和上海市科委基金项目(03Dz19504)
  • 【文献出处】 中国新药杂志 ,Chinese New Drugs Journal , 编辑部邮箱 ,2004年09期
  • 【分类号】R94
  • 【被引频次】14
  • 【下载频次】428
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