卡铂热敏脂质体释药特性考察

 目的建立卡铂热敏脂质体包封率和含量测定方法,并对其体外热敏释药特性进行考察。方法采用超滤法分离载药脂质体和游离药物,以甲醇-水作为流动相,采用C₈柱,用HPLC测定包封率。采用超滤分离法考察脂质体在42℃的体外释放规律和不同温度条件下的释放度。结果超滤分离方法的药物回收率为99.5%,加样回收率为100.6%,药物含量测定方法的工作曲线为A=8 572.6ρ-918.77(n=6),r=0.999 9,线性范围0.517～51.7 mg·L^-1;脂质体在42℃条件下的释放规律符合一级动力学过程。结论本方法简便、准确,可以用于测定卡铂脂质体的含量和包封率,所制备的热敏脂质体具有显著的热敏释药特性。

In Vitro of Release Property Carboplatin Thermo-Sensitive Liposome

OBJECTIVE To establish a method for determining carboplatin content and entrapment efficiency of thermo-sensitive liposomes and to study temperature-sensitive release property in vitro.METHODS The liposomes and free drug were separated by ultra filtration.The mobile phase consisted of 15% methanol and 85% water.RP-HPLC was used to determine the entrapment efficiency and content.The release behavior at 42 ℃ and the release rate at different temperatures were studied by ultra filtration method.RESULTS The drug recovery and the sample recovery of ultra filtration were 99.5% and 100.6%.The equation was A=8 572.6ρ-918.77(n=6).A good linearity was obtained in the range of 0.517～51.7 mg·L^-1.The correlation coefficient was 0.999 9.The release property at 42 ℃ in vitro was discribed by the first order model.CONCLUSION The method is convenient,accurate and suitable for determining the content and entrapment efficiency of carboplatin liposomes.Carboplatin liposomes are temperature-sensitive remarkably.