pH值响应聚乙二醇化壳聚糖基隐形纳米胶束的制备及其载药性能  

p H-responsive PEGylated nanoparticles based on dilauryl chitosan:Preparation,physicochemical characterization and in vitro evaluation

作　　者：姚文杰[1] 辛梅华[1] 李明春[1] 方江海[1] 

机构地区：[1]华侨大学材料科学与工程学院,环境友好功能材料教育部工程研究中心,福建厦门361021

出　　处：《化工进展》2015年第1期173-177,223,共6页Chemical Industry and Engineering Progress

基　　金：福建省重点科技项目(2009H0030);福建省自然科学基金(2011J01312和2012J01396);科技部科技人员服务企业(2009GJC40030)项目

摘　　要：聚乙二醇单甲醚（m PEG）先经过氯乙酸羧化后,再通过酰化反应接枝到双烷基壳聚糖上,制备高接枝度的N,N-双十二烷基-3,6-O-m PEG-壳聚糖（PEDLCS）双亲性衍生物,用1H NMR、FTIR、EA等对产物进行表征,并用透析法制得PEDLCS载酮洛芬（KP）胶束。结果表明,PEDLCS在水溶液中能自组装形成胶束,CMC值为0.1170mg/m L;载药胶束的最优投料比为KP/PEDLCS=0.8∶1,载药量34.48%,包封率65.78%,粒径155.1nm,Zeta电位-31.6m V。载药胶束在不同p H值条件下的响应性实验表明,随着p H值的减小,胶束的稳定性降低,胶束粒径变大,具有可逆性。p H值响应范围符合肿瘤细胞微环境（p H值为7.2∽6.0）,有望成为具有p H值响应主动靶向的隐形纳米胶束。Through acylation reaction, a novel chitosan amphiphilic derivative, N,N-dilauryl-3,6-O-m PEG-chitosan（PEDLCS） with high degree of grafting was synthesized by grafting m PEG-COOH onto N,N-dilauryl chitosan. The product was characterized with 1H NMR,FTIR,and EA. KP-loaded PEDLCS micelles were prepared by dialysis. PEDLCS could form micelles via self-assembly in aqueous solution and the CMC value of PEDLCS was 0.1170 mg/m L. The drug loading content and efficiency of KP-loaded PEDLCS micelles were determined as 34.48% and 65.78% respectively under the optimal ratio of KP and PEDLCS（0.8∶1）. The KP-loaded PEDLCS micelles had average size of 155.1nm and zeta potential of-31.6 m V. The response experiments about drug-loaded micelle under the conditions of different p H values showed that stability of the micelles decreased and diameter of the micelles increased with decreasing p H value,and the process was reversible. The range of p H response rightly agreed with the growth microenvironment of tumor cell（p H7.2—6.0）. It would be expected to become a new material of drug delivery system.

关 键 词：两亲性壳聚糖 聚乙二醇单甲醚 p H值响应性 自组装胶束 

分 类 号：O636.1[理学—高分子化学]