文献类型：期刊文献

中文题名：可用于电子顺磁共振检测的pH响应载药胶束的制备与体外评价

英文题名：EPR-Detectable and pH-Responsive Drug-Loaded Micelles:Preparation and in vitro Evaluation

作者：王兆东[1];史炉炉[1];赵红莉[1];洪亚云[1];周丽芳[2];蓝闽波[1,2]

机构：[1]华东理工大学化学与分子工程学院,上海市功能性材料化学重点实验室,上海200237;[2]华东理工大学分析测试中心,上海200237

年份：2019

卷号：45

期号：6

起止页码：910

中文期刊名：华东理工大学学报（自然科学版）

外文期刊名：Journal of East China University of Science and Technology

收录：CSTPCD;;Scopus;北大核心:【北大核心2017】；CSCD:【CSCD_E2019_2020】；

基金：上海市科委“科技创新行动计划”（15441904100）

语种：中文

中文关键词：2,2,6,6-四甲基哌啶氮氧化物(TEMPO);电子顺磁共振;pH响应;载药胶束

外文关键词：2,2,6,6-tetramethylpiperidine-1-oxyl(TEMPO);electron paramagnetic resonance(EPR);pH-response;drug-loaded micelles

摘要：基于乙炔聚合反应,以席夫碱作为酸响应基团,合成了含有2,2,6,6-四甲基哌啶氮氧化物(TEMPO)自由基的pH响应聚合物PA-pH-TEMPO,利用核磁共振氢谱(~1H-NMR)、傅里叶变换红外光谱(FT-IR)、电子顺磁共振波谱(EPR)等对其分子结构进行了表征;以广谱抗肿瘤药物阿霉素(DOX)为模型药物,通过透析法制得了载DOX的胶束DOX@PA-pH-TEMPO。结果表明,PA-pH-TEMPO在对小鼠成纤维细胞L929和人子宫癌细胞HeLa的毒性测试中,没有明显的细胞毒性;DOX@PA-pH-TEMPO胶束的载药量和包封率分别为2.58%和32.09%,表现出良好的pH响应特性和缓释性能,且对HeLa肿瘤细胞具有较强的抑制效果。对PA-pHTEMPO和DOX@PA-pH-TEMPO的体外细胞摄取实验表明,HeLa细胞对材料具有良好的摄取效果,并可检测到明显的EPR信号。
pH-Responsive micelle(PA-pH-TEMPO) modified by 2,2,6,6-tetramethylpiperidine-1-oxyl(TEMPO)was prepared via polymerization of acetylene using Schiff base as acid responsive group. The structure of the PA-pHTEMPO was characterized by 1 H-nuclear magnetic resonance(1 H-NMR), Fourier transform infrared(FT-IR) and electron paramagnetic resonance(EPR), respectively. Furthermore, doxorubicin(DOX), model anticancer drug, was encapsulated in the PA-pH-TEMPO to form DOX-loaded micelles(DOX@PA-pH-TEMPO) through a membrane dialysis method. The results of the experiments showed that the PA-pH-TEMPO had no significant cytotoxicity against L929 and HeLa cells. And the drug loading content and drug entrapment efficiency of the DOX@PA-pH-TEMPO micelles were determined to be 2.58% and 32.09%, respectively. The DOX@PA-pH-TEMPO micelles exhibited obvious pH responsiveness and sustained release properties, and showed a strong inhibitory effect on HeLa cells. The in vitro cellular uptake experiments of PA-pH-TEMPO and DOX@PA-pH-TEMPO demonstrated that HeLa cells showed good uptake against these materials, and an obvious EPR signal could be detected.