刺激响应型脂质体在靶向药物递送系统中应用  

Research Advances on Stimuli-responsive Liposomes in the Targeted Drug Delivery System

作　　者：杨治中 王梓亭 魏鹏 YANG Zhi-Zhong;WANG Zi-Ting;WEI Peng(School of Traditional Chinese Medicine,Beijing University of Chinese Medicine,Beijing 100029,China;Dongzhimen Hospital,Beijing University of Chinese Medicine,Beijing 100700,China)

机构地区：[1]北京中医药大学中医学院,北京100029 [2]北京中医药大学第一临床医学院,北京100700

出　　处：《中国生物化学与分子生物学报》2020年第12期1395-1403,共9页Chinese Journal of Biochemistry and Molecular Biology

基　　金：国家自然科学基金项目(No.31800652)资助。

摘　　要：脂质体作为一种纳米载体,因低毒性、良好的生物相容性和生物降解性等优势已广泛应用于药物递送系统,但目前脂质体药物仍存在药物释放缓慢、靶向性低、生物利用度不足等问题。因此,引入刺激响应型脂质体这类新型药物递送系统尤为关键,以期有效提高药物靶向性、摄取率和生物利用度,并减少药物毒副作用。刺激响应型脂质体可在循环系统及正常组织或细胞内保持结构稳定,递送至目标部位后,则可在相应内外部刺激条件下被激活,释放运载物,从而对目标部位进行精准治疗。本文重点介绍pH敏感型脂质体和热敏脂质体两类刺激响应型脂质体的设计、作用原理与近期研究应用,讨论有关脂质体常见的靶向修饰方法,并对刺激响应型脂质体在药物递送领域仍面临的问题与发展前景作概括展望。Liposome,a kind of nanoscale vesicle,is applied in the drug delivery systems(DDS)extensively because of its low toxicity,biodegradability and biocompatibility.However,defects of liposome drugs,such as low rates of drug release,insufficiency in active targeting and inefficient bioavailability still remain to be solved.Therefore,stimuli-responsive liposomes are brought to DDS to improve the efficacy of controlled drug release,assure specific release in targeted sites and alleviate side-effects as much as possible.Stimuli-responsive liposomes could maintain stability in circulation,tissues and cells under physiological conditions.Once delivered,they could be activated by relevant internal or external stimuli to release cargos accurately in target areas.This review highlights the design,functional principles and recent advances on application of pH-sensitive liposomes and thermosensitive liposomes respectively,which are two typical stimuli-responsive liposomes.Common targeting modifications of liposomes are discussed as well.We also summarize recent challenges of stimuli-responsive liposomes and their further applications.

关 键 词：pH敏感型脂质体 热敏脂质体 刺激响应 药物递送系统 

分 类 号：R94[医药卫生—药剂学] TQ460.1[医药卫生—药学]