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盐酸米托蒽醌多囊脂质体的制备工艺优化及性能

刘源岗1,2,郑琪瑶1,王士斌1,2   

  1. 1华侨大学化工学院,福建 厦门 361021;2华侨大学制药工程研究所,福建 厦门 361021
  • 出版日期:2013-06-05 发布日期:2013-06-05

Preparation optimization and characterization of DHAD loaded multivesicular liposomes

LIU Yuangang1,2,ZHENG Qiyao1,WANG Shibin1,2   

  1. 1College of Chemical Engineering,Huaqiao University,Xiamen 361021,Fujian,China;2Institutes of Pharmaceutical Engineering,Huaqiao University,Xiamen 361021,Fujian,China
  • Online:2013-06-05 Published:2013-06-05

摘要: 采用均匀设计优化并制备了平均粒径为58.75 μm的载盐酸米托蒽醌多囊脂质体。该多囊脂质体粒度分布较窄,球形度好。Zeta电位、相变温度及稳定性考察均表明该体系稳定性强,适于药物的释放体系。渗漏率结果表明相对于室温(37 ℃),冰箱(4 ℃)更有利于载药多囊脂质体的保存。盐酸米托蒽醌平均包封率为90.13%,考察了胆固醇及三油酸甘油酯用量对多囊脂质体药物释放的影响,药物释放符合《药典》规定,无突释效应,且具有较好的体外缓释性能。

关键词: 盐酸米托蒽醌, 多囊脂质体, 均匀设计, 稳定性, 缓释

Abstract: DHAD loaded multivesicular liposomes (DHAD-MVLs) with the mean diameter of 58.75 μm were prepared using uniform design. The DHAD-MVLs showed narrow particle size distribution and good sphericity. Zeta potential,DSC and drug stability test all revealed that this system was stable and fit for drug delivery system. Leakage rate results indicated that 4℃ was better for drug-loaded MVLs storage compared to 37℃. The average encapsulation efficiency of DHAD was 90.13%. Finally,the influences of cholesterol and trioleate contents on cumulative release were investigated. All groups were in accord with the China Pharmacopoeia 2010,which meant that there were no burst release and the DHAD-MVLs showed better sustained release in vitro.

Key words: mitoxantrone hydrochloride(DHAD), multivesicular liposomes(MVLs), uniform design, stability, sustained release

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