摘要
以羧甲基壳聚糖(CMCS)为载体,以塞来昔布(Celecoxib)作为模型药物,制备出两亲性的高分子前药,经自组装形成纳米胶束。采用核磁共振氢谱(1H-NMR)和红外光谱图(FT-IR)对原料、中间产物和目标产物的结构进行表征。CMCS-Celecoxib前药的载药量为12.45%,纳米粒的粒径约为200nm,PDI为0.15。纳米粒具有pH敏感性,在pH=5.0的PBS缓冲液中,48h累计药物释放百分率达到了69%。CMCS-Celecoxib纳米粒对肿瘤细胞的抑制作用都表现出良好的剂量依赖性及时间依赖性。
We prepared amphiphilic polymeric prodrugs by chemical synthesis,with the carboxymethyl chitosan(CMCS)as the carrier and the celecoxib as the model drug.The structure of raw materials,intermediate products and target products were characterized by the nuclear magnetic resonance hydrogen spectroscopy(1 H-NMR)and the infrared spectroscopy(FT-IR).The amphiphilic polymeric prodrugs can self-assemble in aqueous media to form unique nanoparticles,with the particle size of 200 nm and the particle size distribution coefficient of 0.15.The drug loading of CMCS-Celecoxib prodrug is 12.45%.It is pH sensitivity,the cumulative drug release percentage achieved 69%in PBS buffer at pH=5.0 after 48 hours of dialysis.CMCS-celecoxib nanoparticles showed both good dose-dependent and time-dependent inhibitory effects on tumor cells.
作者
柯鹏振
李佳明
韩磊
詹斯文
张雪琼
邱彤
KE Peng-zheng;LI Jia-ming;HAN Lei;ZHAN Si-wen;ZHANG Xue-qiong;QIU Tong(Hubei Environmental Monitoring Station,Wuhan 430071,China;,School of Materials Science and Engineering,Wuhan University of Technology,Wuhan 430070,China;School of Chemistry,Chemical Engineering and Life Science,Wuhan University of Technology,Wuhan 430070,China)
出处
《武汉理工大学学报》
CAS
北大核心
2020年第9期20-28,共9页
Journal of Wuhan University of Technology
基金
国家自然科学基金青年基金(31300791)
关键词
羧甲基壳聚糖
塞来昔布
纳米粒
细胞评价
carboxymethyl chitosan
celecoxib
nanoparticles
bioactivity assessment
