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目的：研究阿霉素前体脂质体［ｄｏｘｏｒｕｂｉｃｉｎ（ＤＲ），ｐｒｏｌｉｐｏｓｏｍｅ（ＰＬ），ＤＲＰＬ］对大鼠心肝毒性及对荷瘤小鼠的抗肿瘤活性。方法：以酶活性变化为指标，结合病理组织学检查，观察药物对大鼠的心肝毒性及荷瘤小鼠的生命延长率和药物的抗肿瘤活性。实验动物分为ＤＲＰＬ组和ＤＲ组，其中２．００，１４０，０９８ｍｇ·ｋｇ１对应剂量观察药物对大鼠的毒性；４，２，１ｍｇ·ｋｇ１对应剂量观察药物的抗肿瘤活性。结果：与ＤＲＰＬ相比，ＤＲ可明显增加大鼠血清ＬＤＨ、ＣＫ、ＧＰＴ及ＧＯＴ的活性，ＤＲＰＬ对大鼠心肌细胞的损伤明显小于ＤＲ。相同剂量间相比ＤＲＰＬ延长腹水型小鼠移植瘤ＥＡＣ、Ｈｅｐｓ的存活天数明显高于ＤＲ。结论：ＤＲＰＬ对大鼠心肝毒性明显小于相同剂量的ＤＲ，ＤＲＰＬ不但保持了ＤＲ的抗肿瘤活性，而且有明显增效作用。
Objective: To study the hepatotoxicity of doxorubicin (DR), proliposome (PL) and DRPL in rats and the anti-tumor activity in tumor-bearing mice. Methods: Changes in enzyme activity as an index combined with histopathological examination to observe the drug on rat heart and liver toxicity and tumor-bearing mice, the life extension and drug anti-tumor activity. Experimental animals were divided into DRPL group and DR group, of which 2.00,1 40,0 98mg · kg 1 corresponding dose observation of the toxicity of the drug in rats; 4,2,1mg · kg 1 corresponding dose observed drug Antitumor activity. Results: Compared with DRPL, DR could obviously increase the activity of LDH, CK, GPT and GOT in rat serum. The damage of DRPL to rat cardiomyocytes was significantly less than that of DR. The survival of Heps was significantly higher than that of DR at the same dose compared with DRPL prolongation of ascites transplanted tumor EAC. Conclusion: The hepatotoxicity of DRPL in rats is obviously lower than that of the same dose of DR. DRPL not only maintains the antitumor activity of DR, but also has obvious synergistic effect.