文献类型：期刊文献

中文题名：化学组成对聚乙二醇化硬脂酰壳寡糖纳米胶束性能的影响

英文题名：Infl uence of Chemical Compositions on the Properties of PEGylated Stearyl Grafted Chitooligosaccharide Nanomicelles

作者：江东波[1];张炜华[1];刘建文[1];沈熊[2];翁伟宇[1]

机构：[1]华东理工大学药学院,上海市新药设计重点实验室,上海200237;[2]复旦大学附属中山医院,上海200032

年份：2014

卷号：45

期号：7

起止页码：634

中文期刊名：中国医药工业杂志

外文期刊名：Chinese Journal of Pharmaceuticals

收录：CSTPCD;;北大核心:【北大核心2011】；CSCD:【CSCD2013_2014】；

基金：上海市科委基金(11DZ2260600)

语种：中文

中文关键词：硬脂酰壳寡糖;聚乙二醇化硬脂酰壳寡糖;胶束性质;细胞生长抑制;药动学

外文关键词：stearyl grafted chitooligosaccharide; PEGylated stearyl grafted chitooligosaccharide; micelle property;cell growth inhibition; pharmacokinetics

摘要：合成了硬脂酰壳寡糖(COS-SA)和聚乙二醇化硬脂酰壳寡糖(PEG-COS-SA),两者在水中均可自组装成纳米胶束。考察了空白胶束和载盐酸多柔比星胶束的性质。结果表明,COS-SA中硬脂酸取代度主要影响临界胶束浓度,与硬脂酸/壳寡糖的投料比呈线性关系;载药胶束的粒径显著大于空白胶束;PEG修饰可进一步使胶束的粒径和临界胶束浓度增大、ζ电位减小。两种载药胶束的释药行为相似,均有明显的缓释作用。与COS-SA载药胶束相比,PEG化载药胶束对肿瘤细胞生长的抑制率较低,但血清稳定性良好,静脉注射后的长循环效果显著。提示化学组成对以壳寡糖衍生物为载体的纳米胶束性能有重要影响。
Stearyl grafted chitooligosaccharide （COS-SA） and its PEGylated derivative （PEG-COS-SA）were synthesized.Both materials could self-assemble into nanomicelles in aqueous solution.The properties of the blank and doxorubicin hydrochloride nonamicelles with COS-SA or PEG-COS-SA as carrier were investigated.The results showed that there was a linear correlation between the substitution degree of stearic acid （SA） in COS-SA and the feed ratio of SA to COS.The substitution degree of SA affected the critical micelle concentration （CMC）.The particle size of the drug-loading nanomicelles was significantly larger than that of the corresponding blank nanomicelles.PEGylation could further increase the particle size and CMC but decrease the ζ potential.Both nanomicelles exhibited sustainedrelease profiles of doxorubicin and no significant differences in the release behavior were observed.Compared with the COS-SA nanomicelles,the PEG-COS-SA nanomicelles showed good serum stability,prolonged circulation time,but low cytotoxicity against tumor cells.It indicated that chemical composition was a decisive factor for the properties of nanomicelles with chitooligosaccharide derivatives as carriers.