植入瘤体内的氟尿嘧啶微球  

FLUOROURACIL MICROSPHERES FOR INTRATUMOR INJECTION

作　　者：陆彬[1] 熊素彬[1] 王建[2] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]四川省肿瘤医院,四川成都610041

出　　处：《药学学报》2002年第12期971-975,共5页Acta Pharmaceutica Sinica

基　　金：卫生部科学研究基金资助项目 ( 98 1 35 2 )

摘　　要：目的　为提高抗癌疗效 ,制备可植入瘤体内的氟尿嘧啶微球。方法　以聚乳酸为载体材料 ,O W型乳化挥发法制备氟尿嘧啶微球 ;考察了微球性质、体外释药及植入实体瘤Lewis肺癌的抑瘤效果。结果　微球载药量为(10 30± 0 2 0 ) %,包封率为 (6 8 3± 1 5 ) %;外观圆整光滑 ,为物理包载 ;突释很少 ,体外释药t1 2 较原药延长约 16 8倍 ,属扩散 溶蚀机制 ;抑瘤率可达 6 0 6 %,降低了毒副作用。结论　O W型乳化挥发法制备的氟尿嘧啶聚乳酸缓释微球 ,植入瘤体内杀灭肿瘤细胞将可能成为肿瘤化疗的有效方法。AIM To prepare sustained release fluorouracil microspheres for intratumor injection increased antitumor effect. METHODS An O/W emulsion-solvent evaporation method was used to prepare fluorouracil sustained release microspheres. The characterization, drug release in vitro and antitumor effect of fluorouracil sustained release microspheres for intratumor injection on solid tumor such as Lewis lung cancer were investigated. RESULTS The drug loading was (10.30±0.20)%, and the encapsulation efficiency was (68.3±1.5)%. The appearance of fluorouracil sustained release microspheres was smooth and spherical. Fluorouracil was physically incorporated with little burst effect. The t 1/2 in vitro release from the microspheres was 168 times longer than fluorouracil, with drug diffusion and polymeric erosion controlled mechanism. The inhibition rate of fluorouracil microspheres was 60.6% and the side effect was reduced. CONCLUSION The prepared fluorouracil sustained release microspheres was shown to be satisfactorily effective to lung cancer. The intratumor injection seems to be a potential chemotherapeutic approach.

关 键 词：氟尿嘧啶 氟尿嘧啶缓释微球 聚乳酸 瘤体 缓释制剂 

分 类 号：R944.9[医药卫生—药剂学] R979.[医药卫生—药学]