设计和开发 IT-101，一种喜树碱的环糊精聚合物缀合物。
Design and development of IT-101, a cyclodextrin-containing polymer conjugate of camptothecin.
机构信息
Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA.
出版信息
Adv Drug Deliv Rev. 2009 Nov 12;61(13):1189-92. doi: 10.1016/j.addr.2009.05.005. Epub 2009 Aug 12.
IT-101 (Insert Therapeutics-101) is a linear, cyclodextrin-containing polymer conjugate of camptothecin (CPT). When formulated properly, the polymer conjugate self-assembles into nanoparticles of ca. 30 nm diameter and near neutral zeta potential. The nanoparticles show long circulation half-lives in animals and humans and localize in tumors. The nanoparticles enter the tumor cells and slowly release the CPT causing them to disassemble into individual polymer chains that are sufficiently small to be cleared renally. IT-101 is currently being investigated in human clinical trials. Here, the design and development of IT-101 is described with emphasis on features distinguishing it from other polymer-containing therapeutics.
IT-101（Insert Therapeutics-101）是喜树碱（CPT）的一种线性、含环糊精的聚合物缀合物。当配方合适时，聚合物缀合物会自组装成约 30nm 直径和近中性 zeta 电位的纳米颗粒。这些纳米颗粒在动物和人体内表现出长循环半衰期，并在肿瘤部位聚集。纳米颗粒进入肿瘤细胞后，会缓慢释放 CPT，导致其分解成足够小的单个聚合物链，从而可以通过肾脏清除。目前正在进行 IT-101 的人体临床试验。本文重点介绍了 IT-101 的设计和开发，强调了其与其他含聚合物治疗剂的区别。
Zotero 插件