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通过酰化反应将亚油酸引入到壳寡糖(COS)中得到两亲性衍生物N-亚油酰壳寡糖(LCOS)。用IR、元素分析和凝胶渗透色谱进行了结构表征。运用芘荧光探针法研究LCOS在水溶液中的胶束化行为,并制备LCOS负载四苯基卟啉(TPP)的载药胶束(TPP-LCOS)。通过等温滴定微量热法(ITC)测定了LCOS对TPP负载过程的热力学参数。结果表明,产物取代度约为42.1%;LCOS的临界胶束质量浓度CMC为2.00×10-3g/L,可有效负载TPP成纳米球形胶束,粒径在60~100 nm。并且LCOS与TPP之间中等强度的结合(Ka=2.87×106L/mol),有望使TPP缓慢释放,增加药效时间。
Linoleic acid was introduced into chitooligosaccharides (COS) by acylation to give the amphiphilic derivative N-linoleyl chitooligosaccharides (LCOS). Structural characterization was performed by IR, elemental analysis and gel permeation chromatography. The micelles of LCOS in aqueous solution were investigated by pyrene fluorescence probe method, and the drug-loaded micelles (TPP-LCOS) of LCOS supported tetraphenylporphyrin (TPP) were prepared. The thermodynamic parameters of the TPOS loading process for TPP were determined by isothermal titration microcalorimetry (ITC). The results showed that the product substitution degree was about 42.1%. The critical micelle concentration of LCOS was 2.00 × 10-3g / L, which could effectively load TPP into spherical nano-micelles with a particle size of 60-100 nm. And the moderate binding between LCOS and TPP (Ka = 2.87 × 106L / mol) is expected to release the TPP slowly and increase the pharmacodynamic time.