克班宁长循环脂质体的包封率、体外释放和稳定性研究

摘要

目的 研究克班宁长循环脂质体的包封率、体外释放和稳定性.方法 建立高效液相色谱法测定长循环脂质体中克班宁的含量;分别采用葡聚糖凝胶柱层析法和超滤离心法分离未包封克班宁,并对包封率和载药量进行测定;采用透析法考察克班宁长循环纳米脂质体的体外释放行为;考察不同温度和光照贮存条件下克班宁长循环脂质体外观、粒径和泄漏率.结果 采用葡萄糖凝胶柱层析法分离游离克班宁测得包封率为79.46％,采用超滤离心法测得包封率为81.02％,克班宁长循环脂质体载药量为5.6％;克班宁长循环脂质体体外释放规律拟合为Higuchi方程:y=0.1419x1/20.1475,R2值为0.9338;在40 d内克班宁长循环脂质体在避光4℃冷藏条件下贮存稳定.结论 超滤离心法操作简单,重现性好,所制得的脂质体具有明显的缓释释放特征,需避光冷藏贮存.%Objective To study the entrapment efficiency,drug release in vitro and stability ot Crebanine long circulating liposome.Methods The concentration of Crebanine in long circulating liposome was determined by high performance liquid chromatography.The liposome and free Crebanine were separated by the sephadex gel column chromatography and the centrifugal ultrafiltration,the entrapment efficiency and drug loading were determined.The release behavior of the drug from liposome was studied by the dialysis method.The liposome appearance,particle size and leakage rate were studied by the effects of different temperature and light storage.Results The entrapment efficiency was 79.46％ by the gel column chromatography and 81.02％ by the centrifugal ultrafiltration.Crebanine long-circulating liposome drug loading was 5.6％;the Higuchi equation of Crebanine long-circulating liposome in vitro release was y =0.1419 x12+ 0.1475,the R2 value was 0.9338;Crebanine long-circulating liposome was stabilized in the avoid light of 4℃ under refrigeration.Conclusion The centrifugal ultrafiltration is simple and reproducible.The prepared liposome is typical sustained-release,the liposome needs to be kept in cold storage.