【作者】 赵玮璇； 卢雪； 周明；

【Author】 ZHAO Wei-xuan;LU Xue;ZHOU Ming;Institute of New Materials and Advanced Manufacturing,Beijing Academy of Science and Technology;Department of Mechanical Engineering,Tsinghua University;

【机构】 北京市科学技术研究院新材料与先进制造研究所； 清华大学机械工程系；

【摘要】 以顺铂药物或其联合应用为基础的化疗是一类常见的肿瘤治疗方法 ,但由于顺铂的非特异性所导致的副作用、小分子药物的药代动力学特征较差、易产生耐药等原因,极大地限制了顺铂作为一线抗肿瘤药物的临床应用。因此,开发低毒、高效的新型药物制剂成为顺铂类药物的研发热点。纳米载体递送可以通过增强渗透性和保留效应实现将抗肿瘤药物输送至肿瘤区域,是目前新兴的药物递送载体。其中脂质体具有靶向、减毒、增效的优良特性,是抗肿瘤药物的理想递送载体。目前,已有多种顺铂脂质体进入临床研究中,包括多室脂质体、长循环脂质体、触发释放脂质体等。本文综述了顺铂药物的基本性质及其临床应用,总结了顺铂作为一线抗肿瘤药物的优缺点及其局限性,并对国内外已进入临床研究的顺铂脂质体处方的临床评价进行了分析,总结了顺铂脂质体药物的特点、优势和未来的主要发展方向,以期为顺铂药物的脂质体化研究提供思路和参考。更多还原

【Abstract】 Cisplatin is a well-known chemotherapeutic drug whose combination chemotherapy is the basis of treatment of many cancers.However,the clinical application of cisplatin drugs faces serious undesirable effects,including dose-limiting toxicity,poor pharmacokinetic characteristics of small molecule drugs and drug resistance.Therefore,the development of new dosage form with low toxicity and high efficiency has become a hot spot in the research and development of cisplatin drugs.Nanocarriers can deliver drugs to tumor areas by enhancing permeability and retention effects,which is one of the most famous drug carriers.Liposomes are novel drug carriers,as they have targetability,innocuity and efficiency.Nowadays,Multiple types of cisplatin liposomes have entered clinical trials,including multivesicular liposome,long-circulating liposomes,and sPLA2 hydrolysable liposomes.This comprehensive review highlights the physicochemical properties of cisplatin and discusses its uses(either alone or in combination with other drugs) for the treatment of various human cancers.We also reviewed the information regarding formulation of Cisplatin liposomes and its analysis in clinical studies,including characteristics,advantages,and future development directions,to provide ideas and references for the study of cisplatin liposomes.更多还原