木香烃内酯与去氢木香内酯共包封聚乙二醇化长循环脂质体的制备及表征

目的优化川木香主要药效成分木香烃内酯(Cos)与去氢木香内酯(DL)共包封的聚乙二醇(PEG)化长循环脂质体的制备工艺,并对其进行表征。方法采用薄膜水化法制备Cos与DL共包封的PEG化长循环脂质体,以包封率为指标,通过单因素考察结合Box-Behnken响应面法对处方进行优化,并对脂质体的形态、粒径及表面电位、包封率、稳定性和体外释放度进行测定。结果最佳制备工艺为药脂比0.14∶1、胆固醇与磷脂比0.05∶1、m PEG-2000-DSPE添加量6%、水化时间30 min、探头超声时间4 min。所得脂质体外观圆整、分散均匀,平均粒径为(104.80±2.48)nm,多分散指数(PDI)为0.245±0.031,Zeta电位(-9.70±0.23)m V,Cos包封率(91.9±2.6)%,DL的包封率(94.41±1.23)%。结论工艺和处方优化后制得外观形态良好、配伍药物包封率均较高的PEG化脂质体。

Preparation and characterization of PEGylated long-circulating liposomes encapsulating costunolide and dehydrocostus lactone

Objective To prepare pegylated long-circulating liposomes co-encapsulated by costunolide (Cos) and dehydrocostus lactone (DL), optimize the formulation and process, and evaluate the quality. Methods The pegylated long-circulating liposomes co-encapsulated by Cos and DL were prepared by film hydration method. Single factor test and Box-Behnken response surface methodology were used to optimize the preparation process with encapsulation efficiency of Cos and DL as the index. The particle size, surface potential, encapsulation efficiency and in vitro release of the liposomes were evaluated. Results The optimal preparation conditions were as follows:drug-to-lipid ratio was 0.14, ratio of cholesterol to phospholipid was 0.05, mPEG-2000-DSPE addition amount was 6%, hydration time was 30 min, and probe ultrasonic time was 4 min. The obtained liposome was round and uniform in distribution, with an average particle size of (104.8 ±2.48) nm, a polydispersity index (PDI) of (0.245 ±0.031), and a Zeta potential of (-9.7 ±0.23) mV, the encapsulation efficiency of Cos and DL were (91.9 ±2.6)% and (94.41 ±1.23)%, respectively. Conclusion The PEGylated long-circulating liposome prepared by the process and prescription optimization has good appearance and high encapsulation efficiency, which can meet the application requirements.