负载光敏剂的壳寡糖衍生物纳米胶束的制备及性能

Preparation and Properties of Photosensitizer-Loaded Chitosan Oligosaccharide Derivative Nano-Micelles

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2.00×10-3 g/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=2.87×106 L/mol），有望使TPP缓慢释放，增加药效时间。

Amphiphilic derivative of chitosan oligosaccharide （COS）, N-linoleyl chitosan oligosaccharide（LCOS） ,was obtained by introducing linoleic acid into COS through acylation reaction. The chemical structure of LCOS was characterized by means of IR, elemental analysis and Gel permeation chromatography（GPC）. The micellization behavior of LCOS in aqueous solution was studied by fluorescence spectroscopy using pyrene as a probe, and the meso-tetraphenylporphyrin-loaded LCOS micelles （TPP-LCOS） were prepared. The thermodynamical parameters of TPP-loaded process were determined by isothermal titration calorimetry （ITC）. The results show that the substitution degree of the product was about 42. 1%. The critical micelle concentration of LCOS was 2.00 × 10^-3 g/L. TPP could be efficiently loaded by LCOS into spherical nano-micelles, and the particle size of the TPP- loaded LCOS micelles was between 60 and 100 nm. In addition, the medium-strength combination between LCOS micelles and TPP（ Ka = 2.87 × 10^6 L/tool） would be expected to slow release of TPP and enhance the efficacy time.