表阿霉素-白藜芦醇长循环脂质体的制备及其体外释放

目的制备经聚乙二醇(PEG)修饰的表阿霉素-白藜芦醇长循环脂质体,考察长循环脂质体体外释药行为,并对其抗肿瘤作用进行评价。方法采用薄膜分散法-硫酸铵梯度法制备表阿霉素-白藜芦醇长循环脂质体;采用动态透析法考察其体外释药行为;SRB法评价体外抗肿瘤作用。结果采用薄膜分散法-硫酸铵梯度法制备的长循环脂质体中表阿霉素与白藜芦醇包封率可达89.80%、65.01%。体外释放研究表明,表阿霉素-白藜芦醇长循环脂质体较普通脂质体及原料药释药速度更慢,稳定性更好。体外细胞毒试验显示,长循环脂质体对C6胶质瘤细胞具有较强的抑制作用。结论制备长循环脂质体操作简便、重复性好,包封率较高,体外释放具有缓释特征,体外抗肿瘤作用强。

Preparation of epirubicin-resveratrol long circulating liposome and its in vitro releasing properties

Objective To study the preparation of PEG-modified epirubicin-resveratrol long circulating liposome and investigate the drug release from liposome and its anticancer effects in vitro. Methods The long circulating liposomes were prepared by film dispersion method-pH gradient method. Its behavior of drug release from liposome in vitro was investigated by dynamic dialysis. Its anticancer effect of long circulating liposome in vitro was studied by SRB. Results Consequently,the encapsulation efficiency of long circulating liposome was 89. 80% and 65. 01%for epirubicin（ EPI） and resveratrol（ RES）. The result of EPI and RES release from long circulating liposomes were more lower and stabile than those of normal liposome and free drug conspicuously. Its cytotoxicity of long circulating liposome was significantly higher than that of normal liposome and free drugs against C6 glioma cell. Conclusion The film dispersion method-pH gradient method is a simple,reproducible,and high drug encapsulation efficiency. Epirubicin-resveratrol long circulating liposome has delayed release and high anticancer effect.