HZ08冻干脂质体的制备及其逆转肿瘤多药耐药的研究

Preparation of lyophilized HZ08 liposomes and the reversal of multidrug resistance in tumor

制备了HZ08冻干脂质体,考察脂质体冻干前后的包封率、粒径和长期放置稳定性等指标。通过K562/A02细胞逆转阿霉素耐药性实验,考察了HZ08冻干脂质体对逆转阿霉素耐药性作用。结果表明:制备的HZ08脂质体冻干前后包封率、粒径等指标基本相同。12周的放置实验,HZ08冻干脂质体的药物渗漏率为未冻干的25.92%,且脂质体粒径的增幅仅为未冻干的12.32%,冻干后的脂质体稳定性显著提高。10,3,1μmol/L HZ08脂质体冻干粉对K562/A02细胞具有不同程度的逆转阿霉素的耐药性作用,其逆转倍数分别为50.87、17.75和2.05。分别于3个月、6个月和12月时,取样测定批量生产的HZ08冻干脂质体的各项指标,各项指标无明显变化。

HZ08 liposomes（HL） and lyophilized HZ08 liposomes（LHL） were prepared and characterized by encapsulation efficiency（EE）,particle size（PS） and long term stability.The effect of LHL on reversal of adriamycin resistance was investigated by K562/A02 cell reversal of adriamycin resistance experiment.It was found that the PS and EE had no significant change after freeze-drying of HL.However,leakage rate of LHL（12.32%） was significantly lower than that of LHL（25.92%） after 12-weeks storage.The effect of LHL on the reversal of adriamycin resistance was investigated by K562/A02 cell reversal with different concentration LHL（10,3,1 μmol/L）,and the reversal fold was 50.87,17.75 and 2.05,respectively.In 3 months,6 months and 12 months,LHL was sampled to determine the quality,and there was no obvious change during the storage.