阿霉素隐形脂质体与普通脂质体的抗肿瘤活性比较

 目的 比较阿霉素隐形脂质体与普通脂质体的抗肿瘤活性。方法 将聚乙二醇-二硬脂酰磷脂酰乙醇胺（PEG-DSPE）同磷脂酰胆碱和胆固醇材料加在一起，用硫酸铵梯度法制备阿霉素隐形脂质体，参照同法制备阿霉素普通脂质体（但脂膜中不含PEG-DSPE）；采用动物移植性肿瘤实验法，用H₂₂小鼠肝癌细胞接种于小鼠右侧腋皮下形成实体瘤，考察阿霉素隐形脂质体和普通脂质体给药后对实体瘤的瘤重抑制率。结果 按 5 mg·kg^-1剂量治疗，第2天给药和第7天给药治疗方案，阿霉素隐形脂质体给药组的瘤重抑制率均显著高于普通脂质体给药组的瘤重抑制率；按 10 mg·kg^-1剂量治疗，隐形脂质体给药组的瘤重抑制率比普通脂质体给药组的瘤重抑制率稍高。结论 同普通脂质体给药组相比，阿霉素隐形脂质体给药组的抗肿瘤活性显著地提高。

Comparison of the antitumour activity between stealth liposomal doxorubicin and regular liposomal doxorubicin

OBJECTIVE To compare the antitumor activity between stealth liposomal doxorubicin and regular liposomal doxorubicin. METHODS The polyethylene glycol-distearoylphosphatidylethanolamine(PEG 2000 -DSPE),phosphatidylcholine (from eggs) and cholesterol were added to prepare the doxorubicin stealth liposomes by ammonium sulfate gradients method.The doxorubicin regular liposomes were made by the same procedure excluding the addition of PEG 2000-DSPE to the membrane of liposomes.The animal model of implantation solid tumor was applied to evaluate the antitumor effectiveness between the stealth liposomes and the regular ones by subcutaneous injection of murine heptocarcinoma cells (H22) into the right limb armpit of white mice. RESULTS The tumor weight inhibition rate of the stealth was significantly higher than that of the regular after implantation of H22 cells and subsequent treatment with the drug dose of 5 mg·kg^-1on the second day and on the seventh day.According to the same treatment scheme,the tumor weight inhibition rate of the stealth was slightly higher than that of the regular with the higher dose of 10 mg·kg^-1. CONCLUSION The antitumor activity of stealth liposomal doxorubicin in vivo is higher than that of the regular.