联载多西紫杉醇和反义寡聚脱氧核糖核苷酸脂质体的制备工艺

Preparation process of liposome loading docetaxel and antisense oligodeoxyribonucleotide

目的研究联载多西紫杉醇(Doc)、反义寡聚脱氧核糖核苷酸(ODN)脂质体的制备工艺。方法采用乙醇注入法制备脂质体,以包封率和粒径为主要评价指标来考察脂质体的制备工艺,采用中心组合实验进一步优化处方;用激光粒度仪测量脂质体的粒径;采用HPLC法测定脂质体中Doc的包封率,将ODN用FITC标记,用荧光分光光度计测量荧光强度以测量ODN的包封率。结果最佳处方为磷脂-总胆固醇(3∶1),DOC药脂比为1∶50,胆固醇(Chol)-阳离子胆固醇(DC-Chol)为2.4∶1,Chol-PEG2000含量8%,Doc包封率为50%～60%,ODN包封率为60%～70%。结论用乙醇注入法成功地制备了双载药脂质体。

OBJECTIVE To study the preparation method of liposome loaded with docetaxel（Doc） and antisense oligodeoxyribonucleotide（ODN）.METHODS The liposomes were prepared by ethanol injection method,evaluated with entrapment efficiency and particle diameter and the center combination design.The particle size was determined by nano series.The entrapment efficiency of Doc was determined by HPLC and ODN was labeled with FITC for the entrapment efficiency determination.RESULTS The optimal formulation was phospholipids-cholesterol（3：1）,the ratio of drug to lipid was 1：50,Chol-DC-Chol（2.4：1）,the content of Chol-PEG2000 was 8%,the entrapment efficiency of Doc and ODN were 50%-60% and 60%-70%,respectively.CONCLUSION The liposome loaded with Doc and ODN was successful prepared by ethanol injection method.