壳聚糖-5-氟尿嘧啶微球的制备  

Preparation of chitosan-5-fluorouracil microspheres

作　　者：李和平[1] 肖华伍[2] 龙姝[1] 肖子丹[1] 阮建明[3] 

机构地区：[1]长沙理工大学化学与环境工程学院,湖南长沙410076 [2]中南大学湘雅医院,湖南长沙410083 [3]中南大学粉末冶金国家重点实验室,湖南长沙410083

出　　处：《长沙理工大学学报（自然科学版）》2006年第4期91-96,共6页Journal of Changsha University of Science and Technology:Natural Science

基　　金：国家"863"计划资助项目(2001AA218011);湖南省自然科学基金资助项目(06JJ20038)

摘　　要：为了制备靶向型药物载体系统，采用超声乳化技术，以5-氟尿嘧啶（5-Fu）为模型药物，液体石蜡为有机分散介质，Span 80为乳化剂，戊二醛为交联剂，对壳聚糖（CS）进行乳化交联，制备了壳聚糖-5-氟尿嘧啶（CS-5-Fu）微球．对超声频率为40 kHz时的制备条件进行了优化，优化条件为：戊二醛用量2 mL，CS浓度1．0％。5-Fu浓度1．0％．采用红外光谱和扫描电子显微镜等对该条件下所得产物的结构和形貌进行了表征，采用紫外-可见光谱对其药物释放性能进行了研究．研究结果表明，CS-5-Fu微球外形为比较规整的球形，粒径在1—4μm之间，分布均匀，包封率为46．7％．在pH=7．2的磷酸盐缓冲溶液中，CS-5-Fu微球在30h内的累积释药率为60．4％,具有明显的缓释作用．In order to prepare the targeting drug-loaded system, chitosan （CS） 5 - fluorouracil （5 -Fu）microspheres were prepared in emulsion by using ultrasonic treatment, glutaraldehyde as cross linking agent,span-80 as emulsifer and paraffin oil as oil phase. The condition of preparation has been optimized. The optimum conditions for preparation were as follows： ultrasonic frequency of 40 kHz, 2 mL glutaraldehyde, 1.0% chitosan and 1.0% 5 - fluorouracil. At these conditions, The CS -5 - Fu microspheres were characterized by IR, UV-Vis and SEM. The IR results indicate that 5 -Fu was loaded. SEM images show that the CS -5 -Fu microspheres are spherical shape with diameter＇ s range from 1 - 4 μm. The encapsulated capacity and drug releasing properties were investigated by UV-vis spectrum. The results indicate that the drug encapsulation efficiency of Chitosan （CS） 5- fluorouracil （5 -Fu） microspheres was 46.7%, and cumulative release percentage in the phosphate buffer （pH = 7.2） solutions was 60.4% in 30 h.

关 键 词：壳聚糖 5-氟尿嘧啶 微球 制备 

分 类 号：R944.27[医药卫生—药剂学] R979.1[医药卫生—药学]