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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 of liposomes containing docetaxel (Doc) and antisense oligodeoxyribonucleotide (ODN). Methods The liposomes were prepared by ethanol injection. The encapsulation efficiency and particle size were used as main evaluation indexes to study the preparation process of liposomes. The center combination experiment was used to optimize the formulation. The particle size of the liposomes was measured by laser particle sizer. The encapsulation efficiency of Doc in liposomes was determined by HPLC. The ODN was labeled with FITC. The fluorescence intensity was measured by fluorescence spectrophotometer to measure the encapsulation efficiency of ODN. Results The best prescription was phospholipid - total cholesterol (3:1), DOC ratio 1:50, Chol - DCDC 2.4:1, Chol PEG 2000 8%, Doc package The encapsulation efficiency is 50% -60%, and the ODN encapsulation efficiency is 60% -70%. Conclusion The double-loaded liposomes were successfully prepared by ethanol injection.