【摘要】 以EDC为偶联剂,将胆固醇接枝到壳聚糖主链的氨基上,得到疏水改性的双亲性壳聚糖(CS-Chol),利用FTIR,1HNMR对其结构进行表征。CS-Chol在水相自组装形成自聚集体,通过荧光探针技术研究其自聚集行为,结果显示制得的自聚集体具有较低的CAC(10-2mgmL)。TEM和DLS测试显示制得的自聚集体为纳米级颗粒,粒径随胆固醇取代度的减小(4.7～1.1)而增大(180～380nm)。用99mTc对纳米颗粒进行放射性标记,并利用SPECT对其在头部和腹腔分布进行分析。耳静脉注射后纳米粒子在粘膜富集区域有一定滞留性,主要是由于壳聚糖具有粘膜特征吸附的性质。更多还原

【Abstract】 Cholesterol hydrophobic-modified chitosan (CS-Chol) were synthesized by coupling cholesterol to the amino groups of chitosan with EDC as catalyzer. The structure of CS-Chol was characterized by FTIR and 1H NMR. CS-Chol formed self-aggregates in water, and the self-aggregate behavior were studied by fluorescence probe technique, the results suggested that the self-aggregates had low critical aggregate concentration about 10 -2mg/mL, which was critical to the stability in vivo. The measurements of transmission electron microscope(TEM) and dynamic light scattering(DLS) indicated that the self-aggregates were nanoparticles, and the diameters increased from 180 to 380 nm with the decrease of substitute degree from 4.7 to 1.1. The nanoparticles were radio-labeled with 99mTc, and their distribution in cephalosome and abdominal cavity was analysized by SPECT. CS-Chol nanoparticles were eliminated from blood and abdominal cavity quickly. Some nanoparticles, however, retained in the mucous membrane rich area after otic vein injection, due to the feature adhesion of chitosan to the mucous membrane.更多还原