主动载药法制备硫酸长春新碱脂质体及其包封率的测定

Preparation of iiposomes entrapped vincristine sulfate by active loading and determination of its entrapment efficiency

目的制备硫酸长春新碱脂质体,建立包封率测定方法。方法采用pH梯度法制备硫酸长春新碱脂质体;以阳离子交换树脂分离脂质体和游离药物;用RP-HPLC测定脂质体的包封率。结果硫酸长春新碱脂质体包封率大于85%;在所建立的色谱条件下硫酸长春新碱与辅料及溶剂峰分离良好;硫酸长春新碱在1.0～12.5mg·L^(-1)内线性关系良好(r=0.9999);精密度和回收率均合格。结论pH梯度法适于制备硫酸长春新碱脂质体,所建立的分析方法准确可靠,简单快速,可以用于硫酸长春新碱脂质体包封率的测定。

OBJECTIVE To prepare vincristine sulfate liposomes and to develop a method for determining its entrapment efficiency.METHODS Vineristine was encapsulated in the liposomes using the pH gradient-dependent remote loading technique. Free vinefisfine and liposomes were separated by cation exchange resin and RP-HPLC was applied to determine the entrapment effieieney. RESULTS The entrapment efficiency of vineristine sulfate liposomes prepared by pH gradient method exceeded 85 %. The RP-HPLC method was validated and vineristine sulfate was well separated. The standard eurve was linear over the range of 1.0～ 12.5 mg· L^-1 with the eorrelation eoeffieient of 0.999 9.CONCLUSION The pH gradient technique is suitable for preparing vineristine sulfate liposomes. This method established in this study for determination of the entrapment efficiency of vineristine sulfate liposomes is simple, rapid and aeeurate.