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目的：研究阿霉素（Ｆ－ＡＤＭ）和脂质体阿霉素（Ｌ－ＡＤＭ）对正常ＮＩＨ小鼠和肝癌腹水型（ＨｃＡＣ）小鼠的毒性。方法：采用卵磷脂、磷脂酸和胆固醇，应用冰冻融解法制成多层脂质体。ＮＩＨ小鼠分为阿霉素和脂质体阿霉素两组。每组分为７．５，１５，２０和３０ｍｇ／ｋｇ４个对应剂量组，尾静脉给药，观察６０ｄ。ＮＩＨ小鼠腹内接种ＨｃＡＣ９６ｈ后分为阿霉素和脂质体阿霉素两组，每组分为９，１５和２０ｍｇ／ｋｇ３个对应剂量组，腹腔内给药。结果：脂质体组动物体重和器官失重明显减轻；血生化变化相对减小；外周血白细胞下降幅度减小，恢复加快；心、肾、胃肠道病理损害减轻；药物的ＬＤ５０从１４．７ｍｇ／ｋｇ提高到２１．９ｍｇ／ｋｇ。在接种肿瘤９６ｈ的延迟治疗组，动物对药物的耐受性下降，毒性死亡率升高。而脂质体组仍有较好疗效，生存期有所延长。结论：脂质体载药后可降低阿霉素的毒性并保留药物的抗肿瘤活性。
Objective: To study the toxicity of doxorubicin (F-ADM) and liposomal doxorubicin (L-ADM) to normal NIH mice and hepatocellular carcinoma ascites (HcAC) mice. Methods: Lecithin, phosphatidic acid and cholesterol were used to make multilamellar liposomes by using freeze thawing method. NIH mice were divided into doxorubicin and liposomal doxorubicin two groups. Each group was 7.5, 15, 20 and 30mg / kg 4 corresponding dose group, tail vein administration, observed 60d. NIH mice were intraperitoneally inoculated with HcAC96h and divided into doxorubicin and liposomal doxorubicin two groups, each group was 9, 15 and 20mg / kg3 corresponding dose group, intraperitoneal administration. Results: The body weight and organ weight loss of the liposome group were significantly reduced; the blood biochemical changes were relatively reduced; the decrease of the peripheral white blood cells was reduced and the recovery was accelerated; the pathological damage of the heart, kidney and gastrointestinal tract was relieved. The LD50 of the drug was 14.7 mg / Kg to 21.9 mg / kg. Delayed treatment group 96h tumor inoculation, animal tolerance to drugs decreased, toxic mortality increased. The liposome group is still good effect, survival has been extended. Conclusion: The liposomes can reduce the toxicity of doxorubicin and retain the anti-tumor activity of the drug.