喷雾干燥法制备鼻用甲氨蝶呤壳聚糖微球及其特性的考察  

Preparation and properties of methotrexate loaded chitosan microspheres for the intranasal administration

作　　者：孙宇[1] 钮萌萌[1] 王佳苗[1] 杨琳琳[1] 马瑞静[1] 崔福德[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2009年第4期260-264,289,共6页Journal of Shenyang Pharmaceutical University

摘　　要：目的以壳聚糖为载体材料，甲氨蝶呤为模型药物，制备鼻腔给药甲氨蝶呤壳聚糖微球。方法采用喷雾干燥法制备甲氨蝶呤壳聚糖微球；采用正交设计优化制备工艺，并对药物的包封率、收率、粒径以及释放行为进行考察。结果优化条件下所得微球粒径分布较为均匀，平均粒径为4．0—5．0μm，制成微球后药物可缓慢释放，符合鼻腔给药的要求。结论该方法适用于甲氨蝶呤壳聚糖微球的制备，壳聚糖是良好的鼻用制剂的载体材料，可用于制备脑部靶向鼻黏膜给药制剂。Objective To study the preparation of methotrexate loaded chitosan microspheres for nasal administration. Methods The chitosan microspheres loaded with methotrexate were prepared by a spray-drying method and orthogonal design was introduced to select optimum preparation condition. Characteristics of the microspheres, such as the entrapment efficiencies, product yield and size distributions were investigated in detail. The in vitro released studies and nasal cilia toxicity were also observed. Results The average diameter of the microspheres was（4.0-5.0）μm with narrow size distribution. The drug release rate from the microspheres can be controlled by modifying the polymer/drug ratios and the cilia irritation of the microsphers was found to be minor. Conclusions Spray drying method is suitable for preparing chitosan microspheres loaded with methotrexate, and chitosan could be considered as a good carder for the nasal delivery system for the brain targeting.

关 键 词：壳聚糖 微球 鼻黏膜 甲氨蝶呤 

分 类 号：R94[医药卫生—药剂学]