关键词: 阿霉素;脂质体;L-α-二软脂酰磷脂酰胆碱

    摘 要:目的 探讨以L-α-二软脂酰磷脂酰胆碱(DPPC)和盐酸阿霉素(ADM)为原料制备的温度敏感阿霉素脂质体(Ts-LADM)的温度控释特性和稳定性. 方法 采用改良逆相蒸发法，以DPPC和ADM为原料制备Ts-LADM，动力学光散射法测定其粒径，以荧光分光光度法检测样本中阿霉素含量，计算包裹率.纯化后的Ts-LADM在不同温度下水浴后经葡聚糖凝胶分离并回收脂质体部分，以酸性乙醇法测定阿霉素的释放量，计算释放率. 结果 Ts-LADM粒径分布范围为0.1～0.43μm，平均粒径0.28μm;平均包裹率为37.3%;在不同温度下测定的药物释放率分别为:40℃以下小于20%，在DPPC的相变温度附近突然升高，41℃和42℃分别为81.4%和81.6%，44℃时降为77.2%.42℃下延长加热时间药物释放率无明显增加(P>0.05).未经纯化的脂质体于常温下避光贮存5wk，测定其药物包裹率及渗漏率无明显改变(P>0.05). 结论 温度敏感阿霉素脂质体具有良好的温度控释特性和稳定性.

    Thermo┐controlled drug┐release characteristics and stability of thermo┐sensitive liposome of ADM

    LIU Tong-Gang TANG Min-Zhang JIN Fa-Guang ZHANG Sheng-Yong KUANG Yong-Qing

    1 Department of Respiratory Disease，Tangdu Hospi-tal，Fourth Military Medical University，Xi'an710038，China，

    2 Department of Chemistry，Faculty of Preclinical Medicine，Fourth Military Medical University，Xi'an710033，China

    Keywords:adriamycin;liposome;DPPC

    Abstract:AIM To explore the thermo-controlled release characteristics and stability of thermo-sensitive liposome of adriamycin(Ts-LADM)prepared with L-α-dipalmitoyl-phos-phatidylcholine(DPPC)and adriamycin(ADM).METHODS Ts-LADM was made by improved reverse phase evapora-tion(REPE)with DPPC and ADM.The vesicle diameter was determined by dynamic light scattering(DLS).Encapsu-lation rate was calculated after measurement of ADM in sam-ples through fluorospectrophotometry.The liposome was re-trieved from purified Ts-LADM through sephadex ......