论文部分内容阅读
合成了胆固醇-聚乙二醇-RGD(CHOL-PEG 2000-RGD),并经1H NMR确证结构。采用pH梯度法制备多柔比星脂质体,再以上述RGD衍生物为配体以后插入法制备RGD修饰脂质体。所得制品平均粒径为(122.5±2.8)nm,电位为(-18.35±0.78)mV,包封率为(95.23±1.14)%,透射电镜显示脂质体形态为类球体。对黑素瘤细胞B16的体外生长抑制试验结果显示,原药、未修饰及经RGD修饰的多柔比星脂质体的IC50分别为0.264、0.191和0.106 g/ml。且经RGD修饰的空白脂质体并无明显的细胞抑制作用。
Cholesterol-polyethylene glycol-RGD (CHOL-PEG 2000-RGD) was synthesized and confirmed by 1H NMR. The pH gradient method was used to prepare doxorubicin liposomes, and then the RGD modified liposomes were prepared by inserting the RGD derivatives as ligands. The average diameter of the product was (122.5 ± 2.8) nm, the potential was (-18.35 ± 0.78) mV, and the entrapment efficiency was (95.23 ± 1.14)%. The morphology of the liposomes was spheroid by transmission electron microscopy. The in vitro growth inhibition test on melanoma B16 showed that the IC50 of the original drug, the unmodified and RGD-modified doxorubicin liposomes were 0.264, 0.191 and 0.106 g / ml, respectively. The blank liposomes modified by RGD showed no significant cytostatic effect.