氧化苦参碱聚氰基丙烯酸正丁酯纳米粒的体外释药及肝脏分布研究

In vitro release and the liver targeting of oxymatrine polybutylcyanoacrylate nanoparticles

摘要: 制备了氧化苦参碱聚氰基丙烯酸正丁酯纳米粒(OM-PBCA-NP)，采用透析法观察OM-PBCA-NP体外释药行为,通过小鼠尾静脉注射氧化苦参碱溶液(OM-SOL)和OM-PBCA-NP,考察两种制剂在血液和肝脏中的分布。结果表明，氧化苦参碱溶液在体外4 h内已释放完全，而OM-PBCA-NP 4 h仅释放出总药量的36.73％；OM-PBCA-NP与氧化苦参碱水溶液小鼠静脉注射后在肝脏中的AUC之比为8.338。结果表明，OM-PBCA-NP不仅可以缓慢释药，而且具有一定的肝靶向性。

Abstract: Oxymatrine (OM) polybutylcyanoacrylate nanoparticles (OM-PBCA-NP) was prepared,and in vitro release of OM-PBCA-NP as well as the liver targeting potentials of OM-PBCA-NP and oxymatrine solution (OM-SOL) were studied in mice. It was found that 100% of OM was released from OM solution in 4 h,but only 36.73％ from OM-PBCA-NP. In the study of tissue distribution of OM-PBCA-NP,there existed 8.338-fold increase in the area under the liver concentration-time curve in comparison to that of OM-SOL. Hence,OM-PBCA-NP sustained drug release and increased the liver targeting significantly.