叶酸偶联壳聚糖载羟基喜树碱纳米药物制剂的体外释药性能  

Drug release performance in vitro of folic acid mediated chitosan nanoparticles loaded with 10-hydroxycamptothecine

作　　者：徐强[1] 

机构地区：[1]郑州大学第一附属医院耳鼻喉科,郑州450052

出　　处：《郑州大学学报（医学版）》2012年第1期81-84,共4页Journal of Zhengzhou University(Medical Sciences)

摘　　要：目的:探讨叶酸偶联壳聚糖载羟基喜树碱纳米药物制剂(FA-NPs)的体外释药性能。方法:按照浆-反向动态透析法进行体外模拟释放实验,建立高效液相色谱法测定药物释放量,观察FA-NPs的体外释药性能。分别考察不同释放介质(人工胃液,人工肠液和pH7.4的PBS)、搅拌速度(50、75和100r/min)和载药纳米粒的粒径(604、250和190nm)条件下FA-NPs的体外释药性能。结果:与pH7.4的PBS条件下的药物释放速率比较,FA-NPs在人工胃液中药物释放速率加快,在人工肠液中减慢,但在3种释放介质中均表现为先快速释放后缓慢释放的现象。在75和100r/min搅拌速度下FA-NPs具有相似的释药曲线,50r/min搅拌速度条件下FA-NPs的累积释放量较前两者降低。随着纳米粒粒径的增大,FA-NPs药物释放速率减慢。250nm粒径的FA-NPs在pH7.4的PBS中的累积释放时间超过40h,符合药物释放Higuchi方程:Q=0.0908t1/2+0.0324(R2=0.9844)。结论:FA-NPs体外表现出明显的先快速后缓慢释药现象,符合临床用药目的;药物的释放受释放介质、粒径大小和对释放介质的搅拌速度的影响。Aim：To explore the drug release characteristics of folic acid mediated chitosan nanoparticles loaded with 10-hydroxycamptothecine（FA-NPs） in vitro.Methods：The drug release characteristics of FA-NPs were observed by pulp-reverse dynamic dialysis method for simulation release in vitro,and high-performance liquid chromatography method for determination of 10-hydroxycamptothecine.The effects of release medium,size of nanoparticles,and stirring speed on drug release were investigated.Release medium was artificial gastric juice,artificial intestinal fluid and PBS（pH7.4）.Stirring speed was 50,75 and 100 r/min.Size of nanoparticles was 604,250 and 190 nm.Results：Compared with that of PBS（pH7.4）,the speed of drug release was accelerated in artificial gastric juice,but slowed in artificial intestinal fluid.The characteristics of drug release in all of the three mediums was first quick and then slow.The curve of drug release under condition of 75 r/min stirring speed was similar to that of 100 r/min,and cumulative drug release contents of FA-NPs under condition of 50 r/min were lower compared with those of 75 r/min and 100 r/min.The drug release speed slowed down with the enlargement of nanoparticle size.Cumulative release time of FA-NPs（250 nm） in pH7.4 PBS was more than 40 h,and accorded with Higuchi equation：Q=0.090 8 t 1/2 ＋0.032 4（R2=0.984 4）.Conclusion：The drug release characteristics of FA-NPs would be in accord with the purpose of clinical use.The drug release performance is influenced by release medium,size of nanoparticles,and stirring speed.

关 键 词：纳米药物 释药性能 羟基喜树碱 叶酸 壳聚糖 

分 类 号：R979.1[医药卫生—药品]