低分子量壳聚糖纳米粒子缓释蛋白质药物性能的研究

低分子量壳聚糖纳米粒子缓释蛋白质药物性能的研究 Studies on Controlled Release of Protein Drugs from Chitosan Nanoparticles with Low Molecular Weight 徐咏梅 XU Yong-mei 1 2 first-author 杜予民 DU Yu-min 1 2 武汉大学资源与环境科学学院 武汉大学资源与环境科学学院 College of Resources and Environmental Sciences, Wuhan University College of Resources and Environmental Sciences, Wuhan University 武汉大学资源与环境科学学院,湖北,武汉,430072 武汉大学资源与环境科学学院,湖北,武汉,430072 低分子量壳聚糖 （LCS）和三聚磷酸钠 （TPP）以一定的浓度和体积配比在室温下搅拌 ,制得了LCS和经聚乙二醇修饰的LCS纳米粒子 .用透射电镜观察纳米粒子的形貌 ,傅立叶红外光谱和X 衍射图谱表征其结构 .并利用牛血清蛋白 （BSA）作蛋白质模型药物 ,研究LCS纳米粒子包封和缓释蛋白质药物的性能 ,包封率达 90 %以上 ,在pH 7.4的磷酸盐缓冲溶液中 ,释放达 1周以上 .并将LCS纳米粒子和高分子量壳聚糖 （HCS）纳米粒子进行对比 ,粒径分别为 2 0nm和 2 10nm ,蛋白质包封率分别为 91.1%和 93.2 % ,8d内总释放率分别为 73.9%和17.6 % .增加聚乙二醇的用量可降低蛋白质的包封率 ,加快释放速度 Chitosan nanoparticles have promising potential application for the administration of therapeutic protein, gene and antigens by various routes. The preparation of chitosan nanoparticles of low molecular weight, based on ionic crosslinking process of chitosan with polyanion sodium tripolyphosphate（TPP）, was performed, which was under a certain concentration and volume ratio and extremely mild condition at room temperature. The morphological examination was performed by transmission electron microscopy （TEM）, FT-IR and X-ray diffraction pattern to characterize the structure of the nanoparticles. The effects of adding PEG in crosslinking medium on the size, encapsulating, loading and release properties of nanoparticles were studied. The results indicate that the nanoparticles have a high BSA encapsulation efficiency, which is about 90%, and provides a slow continuous release for the entrapped protein using bovine serum albumin （BSA） as a model protein drug. BSA release is up to 8 days in pH 7.4 phosphate buffer saline. Chitosan nanoparticles with low and high molecular weight are about 20 nm and 210 nm in size, 91.1% and 93.2% in encapsulation efficiency of BSA, 73.9% and 17.6% in total release percent in 8 days respectively. Adding PEG decreases encapsulation efficiency of BSA and accelerates release rate. 壳聚糖 纳米粒子 蛋白质载体 缓释 chitosan nanoparticles protein carriers controlled release TQ460 国家自然科学基金资助项目 （2 99770 14 ） 2003-04-01 2021-04-01 4