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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。
COS-SA and PEG-COS-SA were synthesized, both of which were self-assembled into nanomicelles in water. The properties of blank micelles and doxorubicin-loaded micelles were investigated. The results showed that the degree of substitution of stearic acid in COS-SA mainly affected the critical micelle concentration, which was linear with the feed ratio of stearic acid / chitooligosaccharides. The particle size of drug-loaded micelles was significantly larger than that of blank micelles. Further micelle size and critical micelle concentration increases, zeta potential decreases. The release behavior of the two drug-loaded micelles is similar, both of them have obvious sustained release effect. Compared with COS-SA drug-loaded micelles, PEGylated drug-loaded micelles had lower inhibition rate on tumor cell growth, but serum stability was good, and the long-circulation effect after intravenous injection was remarkable. It is suggested that the chemical composition has an important influence on the performance of nanomicelles supported by chitooligosaccharide derivatives.