不同分散介质对壳聚糖载药微球缓释性能的影响  

Effect of different dispersing media on sustained-release property of chitosan microspheres

作　　者：顾志鹏[1] 李华[1] 蒋丽阳[1] 杨超[1] 翟天亮[1] 万昌秀[1] 

机构地区：[1]四川大学高分子科学与工程学院,四川省成都市610065

出　　处：《中国组织工程研究与临床康复》2009年第21期4128-4132,共5页Journal of Clinical Rehabilitative Tissue Engineering Research

摘　　要：背景:壳聚糖因其具有独特的物理、化学及生物学特性,目前已经成为制备缓释和控释制剂十分理想的天然高分子材料,且壳聚糖微球作为药物缓释形式也受到越来越多的关注。目的:观察液体石蜡和苯甲酸乙酯作为分散介质对壳聚糖载药微球缓释性能的影响。设计、时间及地点:对比观察,于2008-03/07在四川大学逸夫楼实验室完成。材料:壳聚糖(Mw=6.5×105,脱乙酰度80%)为上海卡博试剂有限公司产品;四环素医用级为武汉天运科技有限公司产品。方法:配制2%醋酸溶解的壳聚糖溶液,置于水浴中搅拌乳化一段时间,再加入配好的壳聚糖溶液继续搅拌一段时间后加入交联剂戊二醛搅拌反应交联,制得用液体石蜡和苯甲酸乙酯作为分散介质的载药壳聚糖微球。主要观察指标:利用红外光谱和扫描电镜观察粒径形态、大小及其体外释药的特性。结果:以石蜡为分散介质制得的微球平均粒径为5.574μm,载药率为38.7%,包封率为78.3%,有效释放时间37d;以苯甲酸乙酯为分散介质的微球平均粒径为254μm,载药率为30.7%,包封率为72.8%,有效释放时间15d。结论:石蜡作为分散介质分散效果更好,粒径大小更符合要求,载药率和包封率高,释放时间长,但苯甲酸乙酯作为分散介质合成后分离更容易些。BACKGROUND： Chitosan becomes an ideal natural macromolecular material due to its special physical, chemical and biological properties. Chitosan as drug sustained-release and controlled-release formulation is getting more and more attention. OBJECTIVE： To study the effects of different dispersing media, such as atolin and ethyl benzoate, on sustained-release properties of chitosan microspheres. DESIGN, TIME AND SETTING： A contrast study was performed at Yifu Laboratory of Sichuan University between March and July 2008. MATERIALS： Chitosan （Mw=6.5×10^5, deacetylation degree 80%） was provided by Shanghai Kabo Reagent Co., Ltd.; tetracycline was provided by Wuhan Tianyun Technology Co., Ltd. METHODS： Chitosan was dissolved in 2% acetic acid, emulsionized in water bath, and mixed with glutaraldehyde. Chitosan microspheres were prepared with atolin and ethyl benzoate. MAIN OUTCOME MEASURES： Particle diameter, size and drug release were detected using infrared spectrum. RESULTS： The average diameter of the microspheres prepared by atolin was 5.574μm, drug loading was 38.;. entrapment efficiency was 78.3%, and the effective releasing time was 37 days. While the average diameter of microspheres prepared by ethyl benzoate was 254μm, drug loading was 30.7%, the entrapment efficiency was 72.8%, and the effective releasing time was 15 days. CONCLUSION： Atolin is better as a dispersing medium, the microspheres making by use of atolin has smaller diameter, higher drug loading, higher entrapment efficiency and the longer effective releasing time. On the contrary, it is more convenient to separate the production when using ethyl benzoate as a dispersing medium.

关 键 词：壳聚糖 微球 分散介质 缓释性能 

分 类 号：R318[医药卫生—生物医学工程]