长循环pH敏感顺铂脂质体的制备和研究进展  

Preparation and research progress of long-circulating and pH-sensitive liposomes containing cisplatin

作　　者：史巍[1] 陆莹 龚锐[2] Shi Wei;Lu Ying;Gong Rui(Department of Hepatobiliary and Pancreatic Surgery;Department of Pharmacy,Second Hospital of Tianjin Medical University,Tianjin 300211,China)

机构地区：[1]天津医科大学第二医院肝胆胰外科,天津市300211 [2]天津医科大学第二医院药学部,天津市300211

出　　处：《中国组织工程研究》2018年第26期4229-4234,共6页Chinese Journal of Tissue Engineering Research

基　　金：天津市卫生和计划生育委员会科技基金(2014KZ109)~~

摘　　要：背景:顺铂具有很高的抗肿瘤活性,但严重的不良反应限制了其临床应用。脂质体给药系统可通过被动和主动靶向策略,避免其对正常细胞的毒性,增强肿瘤细胞内的药物浓度。目的:综述长循环pH敏感顺铂脂质体的制备及应用研究进展。方法:以"长循环pH敏感顺铂脂质体;纳米载体;肿瘤治疗;生物毒性"或"long-circulating;pH-sensitive liposomes containing cisplatin;nanocarriers;treatment of tumors;biological toxicity"为检索词,检索万方、爱思维尔数据库和Pub Med数据库中关于长循环pH敏感顺铂脂质体的文章。结果与结论:目前多采用冻干再水化法和逆向蒸发法制备长循环pH敏感顺铂脂质体,其中逆向蒸发法已被证明是最适合的方法,因为其制备的脂质体载体粒径小,可形成纯化的长循环pH敏感顺铂脂质体最终产物。长循环pH敏感顺铂脂质体改进了顺铂的药代动力学,减少了其生物毒性,且具有肿瘤细胞局部定位特性。在胰腺肿瘤小鼠模型实验中,长循环pH敏感顺铂脂质体给药系统与以往传统顺铂静脉给药方法相比具有明显优势,表明这种纳米载体给药系统在未来抗肿瘤治疗应用中具有极佳的前景。BACKGROUND： Although cisplatin is a widely used anticancer agent with a high antitumor activity, its clinical use is limited due to its severe side effects. Liposomes can avoid toxicity to normal cells by using both passive and active targeting strategies, and thus enhance the intracellular concentration of drugs in cancer cells. OBJECTIVE： To review the preparation and application of long-circulating and pH-sensitive liposomes containingcisplatin. METHODS： The authors retrieved the articles about the preparation of long-circulating and pH-sensitive liposomes containing cisplatin in in WanFang, Elsevier and PubMed databases by the keywords as follows： “long-circulating; pH-sensitive liposomes containing cisplatin; nanocarriers; treatment of tumors; biological toxicity” in Chinese and English, respectively. RESULTS AND CONCLUSION： At present, long circulating and pH-sensitive liposomes containing cisplatin are mainly prepared by freeze-thaw and dehydration-rehydration and reverse-phase evaporation. However, reverse-phase evaporation has been proved to be the most suitable method, which can be used to prepare small-size liposome carriers, and the purified long-circulating and pH-sensitive liposome containing cisplatin is finally produced. The long-circulating and pH-sensitive liposome containing cisplatin improves the pharmacokinetics of cisplatin, reduces the biological toxicity, and can localize tumor cells. In the mouse model of pancreatic tumor, this new nano-scaled drug delivery system has obvious advantages compared with the traditional method of cisplatin intravenous administration, which shows a great prospect in the future application of antitumor therapy.

关 键 词：长循环pH敏感脂质体 药代动力学 抗肿瘤疗效 生物毒性 生物材料 

分 类 号：R318[医药卫生—生物医学工程]