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- L ADM)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- L ADM,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- L ADM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- L ADM粒径分布范围为 0 .1～ 0 .4 3μm,平均粒径 0 .2 8μm;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 :4 0℃以下小于 2 0 % ,在 DPPC的相变温度附近突然升高 ,4 1℃和 4 2℃分别为 81.4 %和 81.6 % ,4 4℃时降为 77.2 % .4 2℃下延长加热时间药物释放率无明显增加 (P>0 .0 5 ) .未经纯化的脂质体于常温下避光贮存 5 wk,测定其药物包裹率及渗漏率无明显改变 (P>0 .0 5 ) .
AIM To explore the thermo controlled release characteristics and stability of thermo sensitive liposome of adriamycin (Ts LADM) prepared with L α dipalmitoyl phosphatidylcholine (DPPC) and adriamycin (ADM). METHODS Ts LADM was made by improved reverse phase evaporation (REPE) with DPPC and ADM. The vesicle diameter was determined by dynamic light scattering (DLS). Encapsulation rate was calculated after measurement of ADM in samples through fluorospectrophotometry. The liposome was retrieved from purified Ts LADM through sephadex, and the release of ADM was determined by means of acidity ethanol technique. RESULTS The vesicle diameter ranged from 0.1 μm to 0.43 μm, with an average of 0.28 μm, and the average encapsulating rate was 37.3%. Measured at different temperatures, the ratio of drug release reached the peak around the phase transition temperature of DPPC, which was 81.4% at 41℃ and 81.6% at 42℃, whereas it was less than 20% under 40℃ and 77.2% above 44℃ respectively, but no further increase was observed when the temperature was maintained at 42℃ ( P > 0.05 ). The encapsulation and leakage of unpurified Ts LADM remained stable ( P >0.05) when it was stored for 5 weeks at room temperature and free from light. CONCLUSION Ts LADM was proved to have good thermo controlled characteristics and stability.
出处
《第四军医大学学报》
北大核心
2002年第13期1225-1227,共3页
Journal of the Fourth Military Medical University
