Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, Sichuan University , Sichuan, People's Republic of China.
Mol Pharm. 2013 Oct 7;10(10):3832-41. doi: 10.1021/mp400303w. Epub 2013 Aug 30.
Pirarubicin (THP) is an effective anthracycline for the treatment of solid tumor. However, its potential side effects are prominent and clinical use is restricted. We aimed to develop a novel pirarubicin-oleic acid complex albumin nanoparticle (THP-OA-AN) in order to reduce the toxicity of THP. Oleic acid, human serum albumin (HSA), and egg yolk lecithin E80 was used to prepare THP-OA-AN. Prepared THP-OA-AN was characterized and animal experiments were conducted to assess its tumor suppression effect, distribution, and toxicity. Comparison between THP and THP-OA-AN showed that, with retained antitumor efficiency, the toxicity of THP-OA-AN is significantly reduced regarding bone marrow suppression, cardiotoxicity, renal toxicity, and gastrointestinal toxicity. This study developed a safe and effective formulation of THP, which has greater potential for clinic use in the tumor therapy.
吡柔比星（THP）是一种有效的治疗实体瘤的蒽环类药物。但其潜在的副作用明显，临床应用受限。本研究旨在开发一种新型吡柔比星-油酸复合白蛋白纳米粒（THP-OA-AN），以降低 THP 的毒性。采用油酸、人血清白蛋白（HSA）和蛋黄卵磷脂 E80 制备 THP-OA-AN。对制备的 THP-OA-AN 进行了表征，并进行了动物实验以评估其肿瘤抑制作用、分布和毒性。THP 和 THP-OA-AN 的比较表明，THP-OA-AN 在保留抗肿瘤效率的同时，骨髓抑制、心脏毒性、肾毒性和胃肠道毒性等毒副作用明显降低。本研究开发了一种安全有效的 THP 制剂，在肿瘤治疗方面具有更大的临床应用潜力。
