【摘要】 为了避免抗乙肝核糖核酸 (iRNA)口服易受RNase降解而失活 ,将其制备成抗乙肝iRNA脂质体前体。采用白细胞粘附抑制试验 (LAI)检测了抗乙肝iRNA脂质体前体体外和小鼠口服后体内生物活性。结果表明 ,抗乙肝iRNA脂质体前体口服给药小鼠可明显抑制白细胞粘附 ;而裸露iRNA和正常肝RNA脂质体前体均无作用 ;抗乙肝iRNA脂质体前体体外活性检测未粘附抑制指数 (NAI % )在 5 3.8%～ 76 .2 %。多批次样品活性检测结果显示稳定性和重复性较好。说明将抗乙肝iRNA制备为脂质体前体可作为有效的口服剂型。更多还原

【Abstract】 Biologic Activity of anti-hepatitis B iRNA wrapped in liposome against enzymolysis by RNase was determined by leukocyte adherence inhibition test in vivo in mice and in vitro. The results indicated that anti-hepatitis B iRNA wrapped in liposome, by oral administration, could obviously inhibit the adherence of leukocyte in mice. Meanwhile, both of the naked anti-hepatitis B iRNA and the control RNA could not. In vitro, the non-adherence inhibition indexes of anti-hepatitis B iRNA wrapped in liposome from various batches were 53.8%～76.2%. These results suggested that anti-hepatitis B iRNA wrapped in liposome might be a prospective oral preparation.更多还原