摘要
首先利用单电子转移活性自由基聚合(SET-LRP)制备了聚甲基醚聚乙二醇丙烯酸酯(PPEGMEA)主链,再通过二异丙基氨基锂(LDA)攫取羰基α-位活泼氢合成了含溴的PPEGMEA-Br,通过亲核取代反应和还原反应两步制备得到了大分子开环聚合引发剂PPEGMEA-NH2.然后采用grafting-from策略,PPEGMEA-NH2引发γ-苄基-L-谷氨酸酯五元环酸酐(BLG-NCA)的开环聚合,合成了结构规整的两亲性接枝共聚物PPEGMEA-g-PBLG.接着,以PPEGMEA-g-PBLG为药物载体,负载了阿霉素(DOX).利用紫外吸收光谱法测定了载药胶束的载药量,载药胶束的载药量最高可达到32.3%,载药胶束的体外药物释放具有很好的药物缓释特性.
The poly[poly（ethylene glycol） methyl ether acrylate] （PPEGMEA） backbone was first prepared by single electron transfer-living radical polymerization （SET-LRP）. The backbone was treated with lithium diisopropylamide （LDA） and 2-bromoisobutyryl bromide at --78 ℃ to give Br-containing PPEGMEA-Br. PPEGMEA-NHz macroinitiator was then prepared by successive substitution and reduction reactions. A series of well-defined PPEGMEA-g-PBLG graft copolymers were synthesized by ring-opening graft polymerization of 7-benzyl-L-glutamate-N-carboxyanhydride （BLG-NCA） via grafting-from technique. A series of doxorubicin （DOX）-loaded polymeric micelles based on PPEGMEA-g-PBLG amphiphilic graft copolymers were prepared. The drug loading content （DLC） was measured by UV and the DLC of polymeric micelles was found to be as high as 32.3%. The drug release in vitro showed good delayed drug release feature.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2013年第12期2520-2527,共8页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金(Nos.81171737
21174158)资助项目~~
关键词
两亲性接枝共聚物
单电子转移活性自由基聚合
阿霉素
药物载体
amphiphilic graft copolymer
single electron transfer-living radical polymerization
doxorubicin
drug carrier
