选择性胆甾化壳聚糖两亲材料的合成及其自聚集现象

Preparation and characteristics of self-aggregated cholesterol modified chitosan nanoparticles

以邻苯二甲酰化壳聚糖(PHCS)为中间体,将胆甾醇琥珀酸酯(CHS)选择性接枝到壳聚糖的6-OH上,再经水合肼脱去N-邻苯二甲酰亚胺基,游离出氨基,获得疏水改性的O-胆甾醇基壳聚糖(O-CHCS)。采用傅立叶红外光谱仪(FT-IR)和核磁共振仪(1HNMR)对产物进行结构表征;通过透析法制备O-CHCS自聚集纳米粒,用透射电镜(TEM)和动态激光粒度分析仪(DLLS)表征了纳米粒的形态、粒径、粒径分布及表面电位;以芘为荧光探针测定O-CHCS的临界胶束浓度(CMC)。结果表明,合成的O-CHCS是一种两亲性化合物,能在水中自聚集形成粒径约337nm,ζ电位为+25.6mV的球形纳米粒,获得的纳米粒具有明显的核壳结构和较低的临界胶束浓度,有望成为疏水性药物或DNA的载体。

Hydrophobically modify chitosan derivative-6-O-cholesterol modified chitosan（O-CHCS）was prepared through a protection-graft-deprotection procedure with phthaloylchitosan（PHCS）as an intermediate.The graft copolymers were characterized by Fourier transform infrared（FT-IR）and proton nuclear magnetic resonance （1 H NMR）.The self-aggregated nanoparticles were analyzed by transmission electron microscopy（TEM）,dynamic laser light scattering（DLLS）and fluorescence spectroscopy.It was found that these nanoparticles were of spherical shape with sizes of about 337nm and had low critical micell concentration（CMC）.These nanoparticles may be used as a potential carrier of DNA and hydrophobic drug.