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目的：研制出能够逃避体内网状内皮细胞吞噬的阿霉素隐形脂质体，并考察其在生物体内的分布以及比较阿霉素隐形脂质体与阿霉素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，同法制备阿霉素普通脂质体（但脂膜中不含PEG-DSPE）；通过尾静脉注射给药，比较隐形脂质体阿霉素、普通脂质体阿霉素和游离型阿霉素（盐酸阿霉素注射液）给药后在小鼠各主要脏器组织和血液中的分布情况；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：通过硫酸铵梯度法制备出了包封率高达95%的阿霉素隐形脂质体；同游离型阿霉素和普通脂质体阿霉素相比，隐形脂质体阿霉素在血液中浓度显著提高，循环时间显著延长，在心脏中分布的浓度显著降低；按 5 mg(kg-1剂量治疗，第二天给药和第七天给药治疗方案，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，隐形脂质体?
OBJECTIVE: To develop inviscid liposomes capable of escaping phagocytosis of reticuloendotheliocytes in vivo and to investigate its distribution in vivo and to compare the antitumor activity of doxorubicin stealth liposomes with doxorubicin liposomes . Methods: Polyethylene glycol-distearoyl phosphatidylethanolamine (PEG-DSPE) was added together with phosphatidylcholine and cholesterol to prepare doxorubicin stealth liposomes by ammonium sulfate gradient method. (But without PEG-DSPE in the lipid membrane); administered by tail vein injection, compared stealth liposomal doxorubicin, ordinary liposomal doxorubicin and free doxorubicin Inoculation of mice) in the distribution of the tissues and blood of the major organs of mice; using animal transplanted tumor experiment, H22 mouse hepatoma cells were inoculated into the right axillary skin of mice to form solid tumors, Adriamycin stealth liposomes and liposomes after administration of solid tumor weight inhibition rate. Results: Adriamycin stealth liposomes with encapsulation efficiency as high as 95% were prepared by ammonium sulfate gradient method. Compared with free doxorubicin and ordinary liposomal doxorubicin, stealth liposomal doxorubicin Blood concentration significantly increased circulation time was significantly prolonged, the distribution of the concentration in the heart was significantly reduced; according to 5 mg (kg-1 dose treatment, the next day and the seventh day of administration of treatment programs, doxorubicin stealth lipids The tumor weight inhibition rate of the body-treated group was significantly higher than that of the conventional liposome-treated group. The inhibition rate of the tumor weight of the stealth liposomal group was 10 mg (kg-1) The tumor weight inhibition rate of the liposome-treated group was slightly higher than that of the liposome-treated group.Conclusion: Compared with the liposome-treated group,