Self-assembly and drug delivery behaviors of a novel thermo-sensitive block glycopolymer  

作　　者：CHEN LiQiong ZHANG LiMing CHEN JianJun YANG Jian LI RongXian 

机构地区：[1]DSAMP Laboratory and PCFM Laboratory, School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China [2]Research Institute of Tsinghua University in Shenzhen, Shenzhen 518057, China

出　　处：《Chinese Science Bulletin》2010年第36期4187-4196,共10页

基　　金：supported by the National Natural Science Foundation of China (30470476, 20676155);Natural Science Foundation of Guang-dong Province, China (06023103)

摘　　要：A novel thermo-sensitive block glycopolymer based on peracetylated maltoheptaose (AcMH) and poly(2-ethyl-2-oxazoline) (PEtOz) was synthesized for the first time and characterized by hydrogen nuclear magnetic resonance (1H NMR) spectroscopy and gel permeation chromatograph (GPC) analyses. To obtain such a block polymer, the dihydroxyl poly(2-ethyl-2-oxazoline) homopolymer (OH-PEtOz-OH) was first synthesized by cationic ring-opening polymerization of 2-ethyl-2-oxazoline (EtOz), and then coupled with the peracetylated maltoheptaose having a free hydroxyl group at the reducing end (AcMH-OH) prepared from β-cyclodextrin. It was found that the obtained block polymer could self-assemble into nanosize spherical micelles with a distinct core-shell structure in aqueous solution triggered by its amphiphilic character without any organic solvent. The model drug indomethacin (IND) was efficiently loaded into the resultant polymeric micelles, which was confirmed by 1H NMR spectra, transmission electron microscope (TEM) and dynamic light scattering (DLS) techniques. The release behavior of IND loaded micelles was well in response to the environmental temperature change. It is suggested that the resulting micelles might be a potential targeted carrier for drug delivery.A novel thermo-sensitive block glycopolymer based on peracetylated maltoheptaose （AcMH） and poly（2-ethyl-2-oxazoline） （PEtOz） was synthesized for the first time and characterized by hydrogen nuclear magnetic resonance （IH NMR） spectroscopy and gel permeation chromatograph （GPC） analyses. To obtain such a block polymer, the dihydroxyl poly（2-ethyl-2-oxazoline） homopolymer （OH-PEtOz-OH） was first synthesized by cationic ring-opening polymerization of 2-ethyl-2-oxazoline （EtOz）, and then coupled with the peracetylated maltoheptaose having a free hydroxyl group at the reducing end （AcMH-OH） prepared from β-cyclodextrin. It was found that the obtained block polymer could self-assemble into nanosize spherical micelles with a distinct core-shell structure in aqueous solution triggered by its amphiphilic character without any organic solvent. The model drug indomethacin （IND） was efficiently loaded into the resultant polymeric micelles, which was confirmed by ^1H NMR spectra, transmission electron microscope （TEM） and dynamic light scattering （DLS） techniques. The release behavior of IND loaded micelles was well in response to the environmental temperature change. It is suggested that the resulting micelles might be a potential targeted carder for drug delivery.

关 键 词：自组装行为 药物输送 温敏 凝胶渗透色谱仪 透射电子显微镜 嵌段聚合物 胶束结构 核磁共振光谱 

分 类 号：O633[理学—高分子化学] TB383[理学—化学]