超滤法测定水不溶性药物香豆素-6 PLGA纳米粒的包封率  

Determination of entrapment efficiency of water insoluble drug coumarin 6-loaded PLGA nanoparticles by ultrafiltration

作　　者：李雪春[1] 董晓旭[1] 张玲玲[1] 付京[1] 倪健[1] 

机构地区：[1]北京中医药大学中药学院,北京100029

出　　处：《中国新药杂志》2016年第13期1538-1542,共5页Chinese Journal of New Drugs

摘　　要：目的：建立超滤法测定水不溶性药物香豆素-6纳米粒包封率的方法。方法：采用HPLC法测定香豆素-6,色谱柱：Merck RP-18柱（15 cm×4.6 mm,5μm）;流动相：乙腈-水（95∶5）,检测波长：448 nm。选用不同溶剂稀释纳米混悬液,超滤法分离纳米粒和游离药物,辅以扫描电镜法观察溶剂对纳米粒表面形态的影响,以及游离药物与纳米粒的分离效果,建立测定香豆素-6纳米粒包封率的方法。结果：建立了香豆素-6的分析方法并应用于包封率的测定。选用1%TPGs稀释纳米混悬液,通过超滤法可以有效分离游离香豆素-6,游离药物测定的回收率为98.47%～99.38%。结论：以1%TPGs为溶媒稀释纳米混悬液,采用超滤法可以有效、准确地测定香豆素-6纳米粒包封率。Objective： To establish a method for the determination of entrapment efficiency of coumarin6-loaded PLGA nanoparticles by ultrafiltration method. Methods： HPLC was used to determine drug content of the nanoparticle suspension. A Merck RP-18 column（ 15 cm × 4. 6 mm,5 μm） was used with an isocratic elution of mobile phase composed of acetonitrile and water in the ratio of 95∶ 5. The VWD detection was set at 448 nm. The nanoparticle suspensions were diluted by different vehicles,and free drugs were then separated by ultrafiltration.The effects of dilution solvents on the nanoparticle morphology were observed by scanning electron microscopy,as well as the separation effect of free drug and nanoparticles. The methodology study and the optimization of determining condition were carried out. Results： The HPLC method for coumarin 6 determination was established and applied.Ultrafiltration of nanoparticle suspensions diluted with 1% TPGs could effectively separate the free drug from nanoparticles. The recovery of free drug was 98. 47% ~ 99. 38%. Conclusion： Ultrafiltration can be used to determine the entrapment efficiency of coumarin 6-loaded PLGA nanoparticles after diluting the nanoparticle suspension with1% TPGs aqueous solution.

关 键 词：香豆素-6 纳米粒 包封率 超滤法 

分 类 号：R943[医药卫生—药剂学]