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目的研究八聚精氨酸(R8)修饰的载紫杉醇脂质体的制备工艺。方法采用有机相反应法,将R8修饰到脂质体表面,并以薄膜分散-探头超声法制备载紫杉醇脂质体,以细胞摄取、粒径、PDI、包封率为主要指标对磷脂/胆固醇、药脂比、水化液种类、R8密度、DSPE-PEG2000密度进行筛选,进一步优化处方。结果最优处方为磷脂-胆固醇2∶1、药脂比1∶40、水化液为PBS(pH6.5)、R8密度5%、DSPE-PEG2000密度3%,所制脂质体的粒径为156±2 nm,PDI=0.25,包封率为80.87%±8.9%。结论成功制备了八聚精氨酸(R8)修饰的载紫杉醇脂质体。
Objective To study the preparation process of paclitaxel liposome modified with octameric arginine (R8). Methods The liposomes were modified by the organic phase reaction method and modified with Lipofectamine 2000. The liposomes were loaded with thin-film dispersive-probe ultrasonography. The effects of phospholipid / cholesterol on the liposomes were determined by cell uptake, particle size, PDI and entrapment efficiency , Lipid ratio, hydration fluid type, R8 density, DSPE-PEG2000 density were screened to further optimize the prescription. Results Optimal prescription was phospholipid-cholesterol 2: 1, lipid-lipid ratio 1:40, hydration solution PBS (pH6.5), R8 density 5%, DSPE-PEG2000 density 3% 156 ± 2 nm, PDI = 0.25, encapsulation efficiency of 80.87% ± 8.9%. Conclusion Eight paclitaxel (R8) modified paclitaxel liposomes were successfully prepared.