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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。
In order to prevent inactivation of anti-HBV RNAi by RNase degradation, it was prepared as an anti-Hepatitis B RNAi precursor. The in vivo bioactivities of anti-Hepatitis B RNAi precursors in vitro and in mice after oral administration were tested using the leukocyte adhesion inhibition test (LAI). The results showed that oral administration of anti-Hepatitis B iRNA liposome precursors can significantly inhibit leukocyte adhesion; naked iRNA and normal liver RNA liposome precursors were no effect; anti-HBV RNAi precursor in vitro activity assay Non-adhesion inhibition index (NAI%) in the 5 3.8% ~ 76 .2%. Test results of multiple batches of samples showed good stability and repeatability. The preparation of anti-Hepatitis B iRNA as a liposome precursor can be used as an effective oral dosage form.