CAJ | 학술논문

为研究抗肿瘤药物与辅药负载于同一药物载体的作用效果,首先以壳寡糖和广谱抗肿瘤药物5-氟尿嘧啶(5-Fu)为原料通过化学键合合成氟尿嘧啶-壳寡糖前体,然后以其为模板通过溶胶-凝胶法制备了同时负载氟尿嘧啶和硒纳米颗粒的壳寡糖微球.采用透射电子显微镜(TEM)、 Zeta 电位仪和红外光谱(IR)对制备的微球进行了表征,结果表明,微球粒径为433 nm,硒纳米颗粒包裹在微球内；对微球包裹药物进行检测发现,5-Fu 装载率为(8.2±0.3)%,硒装载率为(7.96±0.34)%；体外缓释检测和细胞实验结果证实,微球能够缓慢释放2种药物,其缓释作用能很好地抑制肝癌细胞 SMMC-7721的生长.
위연구항종류약물여보약부재우동일약물재체적작용효과,수선이각과당화엄보항종류약물5-불뇨밀정(5-Fu)위원료통과화학건합합성불뇨밀정-각과당전체,연후이기위모판통과용효-응효법제비료동시부재불뇨밀정화서납미과립적각과당미구.채용투사전자현미경(TEM)、 Zeta 전위의화홍외광보(IR)대제비적미구진행료표정,결과표명,미구립경위433 nm,서납미과립포과재미구내；대미구포과약물진행검측발현,5-Fu 장재솔위(8.2±0.3)%,서장재솔위(7.96±0.34)%；체외완석검측화세포실험결과증실,미구능구완만석방2충약물,기완석작용능흔호지억제간암세포 SMMC-7721적생장.
5-Fu-COS / SeNP micro-spheres were prepared in two steps to study the antitumor drug load and auxiliary same effects as the drug carrier. First, the Fu-COS prodrug was synthesized with the broad-spectrum anti-tumor drug 5-fluorouracil(5-Fu) and chito-oligosaccharides(COS), then, Fu-COS was used as temples while 5-Fu-COS / SeNP was prepared by sol-gel method. 5-Fu-COS / SeNP was characterized by TEM, Zeta-sizer and IR, and its anti-tumor activity was detected by MTT method. The results showed that 5-Fu and Se were completely carried in 5-Fu-COS / SeNP, the size of 5-Fu-COS / SeNP was 433 nm, the drug-loading rate of 5-Fu and Se were (8. 2±0. 3)% and (7. 96±0. 34)% , respectively, and 5-Fu and nanose released slowly and had well inhibiting tumorous cellular growths activity. As time increases, release rate of the drug by Fu-COS / SeNP increased and the inhibition of cell enhanced. After 24 h, inhibition rate had exceeded the sum of 5-Fu and SeNP. After 48 h, the inhibition rate of Fu-COS / SeNP was less than the sum of the inhibition rate of 5-Fu and SeNP, but higher than that of 5-Fu or SeNP. These results indicated that the spheres have high drug loading efficiency and good drug release properties. This novel method to produce micro-spheres could expand the development of drug release research.