【摘要】 目的研究反义寡核苷酸的聚赖氨酸修饰物对脂质体包封率的影响及对HepG2细胞活性的初步测定。方法利用反义药物的聚赖氨酸修饰物,采用薄膜分散法制备反义寡核苷酸及其聚赖氨酸修饰物的脂质体;紫外分光光度法测定包封率的差异并考察对HepG2细胞细胞毒活性的影响。结果高密度正电荷的聚赖氨酸与带负电荷的反义寡核苷酸偶联后,脂质体的载药量大大增加,并且细胞的摄入量增加,对HepG2细胞生长具有抑制作用。结论聚赖氨酸修饰物增加了反义寡核苷酸的脂质体包封率,有效诱导人肝癌细胞的凋亡作用。更多还原

【Abstract】 Objective To research the effect of poly(L-lysine)conjugated ODN on entrapment rate of N-SLBA liposomes and its inhibition on the proliferation of HepG2 cells.Methods ODNs covalent linkage to poly(L-lysine),preparation of N-SLBA liposomal ODN and N-SLBA liposomal poly(L-lysine)conjugated ODN,encapsulated ODN,poly(L-lysine)conjugated ODN were determined by direct measurement using LC-10 UV instrument,poly(L-lysine)conjugated ODN encapsulated in N-SLBA liposomes inhibited the proliferation of HepG2 cells.Results Amino groups in poly(L-lysine) neutralized negative charges in ODNs and reduced repulsion with liposomal membrane.Effective HepG2 cell transfection could be achieved with the improved entrapment ratio and inhibition on HepG2 cell growth.Conclusions poly(L-lysine)modification of ODN encapsulated in target liposomes improves the encapsulation efficiency and increase the apoptosis of HepG2 cells.更多还原