雷西莫特抗肿瘤纳米给药系统研究进展  

Research progress on nanoscale drug delivery system of resiquimod for tumor treatment

作　　者：李朋鑫 王小欢 宫婷婷 王向涛 LI Peng-xin;WANG Xiao-huan;GONG Ting-ting;WANG Xiang-tao(School of Pharmacy,Henan University of Chinese Medicine,Zhengzhou 450046,China;Instituteof Medicinal Plant Development,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100193,China)

机构地区：[1]河南中医药大学药学院,河南郑州450046 [2]中国医学科学院,北京协和医学院药用植物研究所,北京100193

出　　处：《药学学报》2025年第3期700-710,共11页Acta Pharmaceutica Sinica

基　　金：中国医学科学院医学与健康创新工程(2021-I2M-1-071)。

摘　　要：雷西莫特(resiquimod,R848)属于咪唑喹啉类小分子化合物,是Toll样受体(Toll-like receptor,TLR)7/8的高效激动剂。R848有很强的免疫激动活性,可以激发多种免疫细胞,调节天然免疫和适应性免疫,是一种极具潜力的免疫佐剂。近年来,研究发现R848自身对多种肿瘤具有直接的抗肿瘤疗效,同时还可与化疗、光热治疗等联用表现出良好的协同作用,因此备受广大研究者关注。然而R848没有肿瘤靶向性,大剂量重复给药可产生全身炎症和自身免疫反应,限制了其临床应用。而纳米给药系统可能是解决这些问题的有效途径,包括脂质体、聚合物纳米粒、生物载体、包合物、有机金属骨架和无机纳米材料,以及基于R848前药或R848衍生物的纳米给药系统。本文对R848的理化性质、免疫调控机制、纳米给药系统进行综述,以期为R848的抗肿瘤研究发展及新药开发提供参考和支持。Resiquimod(R848)belongs to the class of weak base organic compounds that are derivatives of imidazole quinoline and is a potent agonist of Toll-like receptor(TLR)7/8.R848 can be considered an effective immune adjuvant as it has the ability to activate different immune cells and regulate innate and adaptive immunity.A number of researches done recently have reported R848 potent anti-tumor capacity,especially when combined with other cytotoxic therapies.Nonetheless,some hurdles remain with the clinical use of R848 such as its limited ability to reach the tumor and likelihood of inflammation and autoimmune responses which might result from repeated delivery of high dosages of the drug.Nanoscale drug delivery systems may overcome some of these challenges.Various nanoformulations,including liposomes,polymeric nanoparticles,biocarriers,inclusion compound,metal-organic frameworks and inorganic nanoparticles,as well as several R848 prodrugs or derivativesbaesd nanoparticles,have been incorporated into present R848 delivery platforms.This article reviews the physicochemical properties,immune regulatory mechanisms and nano drug delivery systems of R848,in order to provide reference and support for anti-tumor research and new drug development.

关 键 词：雷西莫特 抗肿瘤 纳米给药系统 Toll样受体激动剂 免疫疗法 

分 类 号：R943[医药卫生—药剂学]