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采用逆相蒸发法制备了姜黄素脂质体。由于透明质酸脂溶性较差,先将其制成磷脂酰衍生物(透明质酸-磷脂酰乙醇胺,HA-DOPE),再用以修饰载药脂质体。所得脂质体的平均包封率为89%,该衍生物与脂质体的结合率为72%。脂质体于4℃保存30 d包封率无明显改变,但结合率有轻微下降。细胞毒性试验显示,游离姜黄素、姜黄素脂质体及修饰后脂质体对高表达CD44受体的人肺腺癌A549细胞的IC50值分别为0.054、0.032和0.021 mol/ml,未修饰和修饰后的姜黄素脂质体对低表达CD44受体的人肝癌HepG2细胞作用相当。
Curcumin liposomes were prepared by reverse phase evaporation. Due to the poor solubility of hyaluronic acid, phosphatidyl derivatives (hyaluronic acid-phosphatidylethanolamine, HA-DOPE) were first prepared and then used to modify drug-loaded liposomes. The average encapsulation efficiency of the obtained liposomes was 89%, and the binding ratio of this derivative to the liposomes was 72%. The encapsulation efficiency of liposomes stored at 4 ℃ for 30 d did not change significantly, but the binding rate decreased slightly. Cytotoxicity assays showed that the IC50 values of free curcumin, curcumin liposomes and modified liposomes on human lung adenocarcinoma A549 cells highly expressing CD44 receptor were 0.054, 0.032 and 0.021 mol / ml, respectively. The unmodified and The modified curcumin liposomes have the same effect on human hepatoma HepG2 cells with low expression of CD44 receptor.