Dipartimento di Scienze del Farmaco, Università di Chieti-Pescara G. d'Annunzio, Via dei Vestini 31, 66100 Chieti, Italy.
Curr Drug Deliv. 2012 Mar;9(2):122-31. doi: 10.2174/156720112800234558.
Camptothecins are a family of alkaloids originally extracted from the Chinese tree Camptotheca acuminata, Nyssaceae, exhibiting a strong activity against colorectal cancer (CRC). CRC is a common malignancy worlwide. Despite significant developments in the treatment of this disease, it still causes considerable morbidity and mortality. Recent advances include both newer cytotoxic chemotherapies and novel biological agents including the more hydrosoluble camptothecin derivative, namely irinotecan. Camptothecin and irinotecan are selective human topoisomerase I inhibitors but their application for curing CRC is compromised by their intrinsic high toxicity, insolubility and instability. Furthermore, pharmacology studies have determined that continuously and prolonged schedules of administration are required. The aim of this work is to review the state of the art of camptothecin and its derivative irinotecan's delivery methods.
喜树碱是一类生物碱，最初从中国的喜树中提取出来，属于蓝果树科，对结直肠癌（CRC）具有很强的活性。CRC 是一种常见的恶性肿瘤，在全世界范围内都有发生。尽管在这种疾病的治疗方面取得了显著的进展，但它仍然导致了相当大的发病率和死亡率。最近的进展包括更新的细胞毒性化疗药物和新型生物制剂，包括水溶性更好的喜树碱衍生物伊立替康。喜树碱和伊立替康是选择性的人拓扑异构酶 I 抑制剂，但由于其内在的高毒性、不溶性和不稳定性，它们在治疗 CRC 方面的应用受到限制。此外，药理学研究已经确定需要连续和延长的给药方案。本工作旨在综述喜树碱及其衍生物伊立替康的传递方法的最新研究进展。
