胆固醇疏水改性壳聚糖自聚集纳米微粒的制备及其动物体内分布研究  

Paration of Self-aggregate Nanoparticles Composed of Cholesterol Hydrophobic-modefied Chitosan and their Destribution in Cephalosome and Abodominal Cavity

作　　者：原续波[1] 顾鸣岐[1] 原艳波 李弘[3] 王来好[2] 盛京[1] 

机构地区：[1]天津大学材料科学与工程学院,天津300072 [2]山西长治医学院附属医院,长治046000 [3]南开大学吸附分离功能高分子材料国家重点实验室,天津300071

出　　处：《高分子通报》2005年第5期122-127,共6页Polymer Bulletin

基　　金：国家自然科学基金青年基金(NO:50301008)

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。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^-2 mg/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.

关 键 词：胆固醇疏水改性壳聚糖(CS-Chol) 自聚集 纳米微粒 放射性标记 体内分布 改性壳聚糖 疏水改性 胆固醇 分布研究 动物体内 纳米微粒 自聚集 ^1H-NMR 制备 

分 类 号：TQ460.1[化学工程—制药化工]