【作者】 刘袖洞； 周火飞； 于炜婷； 马小军；

【Author】 Xiu-Dong Liu~(1,2,*),Huo-Fei Zhou~2,Wei-Ting Yu~2,Xiao-Jun Ma~(2,*) 1 Dalian University,116622;2 Dalian Institute of Chemical Physics,CAS,116023,Dalian

【机构】 大连大学； 中国科学院大连化学物理研究所；

【摘要】 壳聚糖(CTS)是天然阳离子多糖,具有无毒、生物相容、可生物降解等优异性能,因而在药物/基因转运释放、组织工程等生物医学领域倍受关注[1]。我们通过对CTS进行化学改性,先后在其分子链上接枝油溶性小分子(如石胆酸、脱氧胆酸)和水溶性小分子(如缩水甘油),合成一系列新型水溶性两亲壳聚糖(CTS-LA-TM,HT-CTS-DCA)。其在水溶液中通过自组装过程很容易形成两亲壳聚糖胶束聚集体(Fig 1,160-210 nm),装载难溶性抗肿瘤药物阿霉素(DOX)的包封率达70%,且实现缓释(Fig2),表现出显著的抗肿瘤活性[2,3]。更多还原

【Abstract】 Chitosan(CTS) is natural positive polysaccharide with properties of nontoxicity,biocompatibility,and biodegradability,which benefits it wide application in drug/gene delivery and tissue engineering[1].We synthesized novel soluble amphiphilic chitosan derivatives by grafting both hydrophobic moieties(e.g. deoxycholic acid) and hydrophilic moieties(e.g.glycidol).They can form micelles by self-assembly in aqueous solution(Fig 1).Doxorubicin(DOX) could be easily encapsulated into amphiphilic CTS micelles and keep a sustained release manner without burst release when exposed to PBS(pH 7.4) at 37℃. Antitumor efficacy results showed significant antitumor activity when MCF-7 cells were incubated with different concentration of amphiphilic CTS micelles.更多还原