载于长循环聚合物胶束中的喜树碱增强抗肿瘤作用。
Enhanced antitumor effect of camptothecin loaded in long-circulating polymeric micelles.
作者信息
Kawano Kumi, Watanabe Masato, Yamamoto Tatsuhiro, Yokoyama Masayuki, Opanasopit Praneet, Okano Teruo, Maitani Yoshie
机构信息
Institute of Medicinal Chemistry, Hoshi University, 2-4-41 Ebara, Tokyo 142-8501, Japan.
出版信息
J Control Release. 2006 May 30;112(3):329-32. doi: 10.1016/j.jconrel.2006.03.012. Epub 2006 Mar 27.
A water-insoluble antitumor agent, camptothecin (CPT) was successfully incorporated into polymeric micelles formed from poly(ethylene glycol)-poly(benzyl aspartate) block copolymers (CPT-loaded polymeric micelles). Antitumor effects and biodistribution of CPT-loaded micelles were evaluated in mice subcutaneously transplanted by colon 26 tumor cells. Tumor growth was significantly inhibited after a single i.v. injection of CPT-loaded polymeric micelles at doses of either 15 or 30 mg/kg. Efficacy of a single high-dose injection was comparable to low dose multiple injections. CPT loaded in polymeric micelles showed prolonged blood circulation and higher accumulation in tumors compared with CPT in solution. Polymeric micelle systems offer a stable and effective platform for cancer chemotherapy with CPT.
一种水不溶性抗肿瘤药物喜树碱（CPT）被成功载入由聚乙二醇-聚（苄基天冬氨酸）嵌段共聚物形成的聚合物胶束中（载药聚合物胶束）。对皮下移植结肠26肿瘤细胞的小鼠评估了载药胶束的抗肿瘤效果和生物分布。静脉内单次注射剂量为15或30mg/kg的载药聚合物胶束后，肿瘤生长受到显著抑制。单次高剂量注射的效果与低剂量多次注射相当。与溶液中的CPT相比，载于聚合物胶束中的CPT显示出更长的血液循环时间和更高的肿瘤蓄积。聚合物胶束系统为CPT癌症化疗提供了一个稳定而有效的平台。
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