肿瘤微环境响应型喜树碱及其衍生物纳米前药的研究进展  

Research progress on camptothecin and its derivative nano-prodrugs based on tumor microenvironment response

作　　者：吴豪 胡茂松 罗利霞 周海嫔[1] 胡建露 夏静 柯仲成[3] 王悦 宋捷[2] WU Hao;HU Mao-song;LUO Li-xia;ZHOU Hai-pin;HU Jian-lu;XIA Jing;KE Zhong-cheng;WANG Yue;SONG Jie(School of Material Science and Chemical Engineering,Chuzhou University,Chuzhou 239000,China;Key Laboratory of New Drug Delivery System of Chinese Materia Medica,Jiangsu Province Academy of Traditional Chinese Medicine,Nanjing 210028,China;Research Center of Chinese Medicine Efficacy and Health Technology,Huangshan University,Huangshan 245041,China)

机构地区：[1]滁州学院材料与化学工程学院,安徽滁州239000 [2]江苏省中医药研究院国家中医药管理局中药释药系统重点研究室,江苏南京210028 [3]黄山学院中药功效与健康技术研究中心,安徽黄山245041

出　　处：《中国中药杂志》2022年第11期2852-2865,共14页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81873055);安徽省自然科学基金面上项目(20080805MH269);全国中医药创新骨干人才培训项目;滁州学院启动基金项目(2020qd50);安徽省创新训练项目(S202110377140);滁州市科技计划项目(2021ZD019)。

摘　　要：纳米前药是现阶段运用最为广泛的纳米制剂之一,在肿瘤治疗方面显示出良好的效果,具有极高的临床应用价值和潜力。其中喜树碱及其衍生物在制备前药治疗肿瘤方面具有广阔的前景。针对肿瘤的特殊微环境情况,包括偏酸性、高浓度活性氧和高浓度谷胱甘肽以及酶浓度等,制备得到了大量的肿瘤微环境响应型喜树碱及其衍生物前药。该文尝试从微环境响应类型和释药特征对其进行分类,结合安全性和临床试验总结归纳喜树碱及其衍生物前药的研究进展,分析存在的问题和不足,希望为喜树碱及其衍生物的发展提供借鉴。Nano-prodrug, one of the most widely used nano-formulation at present, has excellent efficacies in tumor treatment with high potential and clinical value. Camptothecin and its derivatives have broad prospects in the preparation of prodrugs for the treatment of tumors. Given the special microenvironment of tumors, including partial acidity, high concentration of reactive oxygen species, high concentration of glutathione and enzyme concentration, a large number of tumor microenvironment-responsive camptothecin and its derivative prodrugs were prepared. This paper classified them from the microenvironment response types and drug release characteristics, reviewed the research progress of camptothecin and its derivative prodrugs based on safety and clinical trials, and analyzed the existing problems and deficiencies, hoping to provide references for the development of camptothecin and its derivatives.

关 键 词：喜树碱 前药 肿瘤微环境 体外释放 

分 类 号：R283.6[医药卫生—中药学]