摘要
目的制备羧甲基壳聚糖载药微粒,对其表面形貌、粒径分布及体外释放等微粒性能进行评估。方法以羧甲基壳聚糖为载体,5-氟尿嘧啶(5-FU)为模型药物,采用乳化交联法制备羧甲基壳聚糖载药微粒,通过电子显微镜观察微粒的外形结构,用紫外分光光度计测微粒的载药量和包封率,并测定体外释放量。结果 5-FU羧甲基壳聚糖载药微粒呈规则球形,平均粒径1～2μm,载药量为17.55%,包封率为45.4%。体外释放实验表明微粒具有缓释特性,在模拟体液中,10 d的累积释药量达94.92%。结论以羧甲基壳聚糖微粒作为5-FU的载体,可改变5-FU在体内的药代动力学行为,具有缓释作用,延长了药物在体内的循环时间,使之发挥更好的抗肿瘤效应。
【Objective】 To prepare the carboxymethylated chitosan microparticle and evaluate its surface morphology,size distribution and drug release properties in vitro.【Methods】 The carboxymethylated chitosan microparticle was used to carry 5-fluorouracil（5-FU） as a model of drug delivery system.The 5-FU-loaded carboxymethylated chitosan microparticles were prepared by the cross-linking emulsion.The particle shape and structure were observed under an electronic microscope.An ultraviolet spectrophotometer was used to measure the drug loading capacity（DL）,the embedding ratio（ER） and the amount of released drug in vitro.【Results】 The carboxymethylated chitosan microparticle was regular and round in shape with the average diameter of 1~2 μm.Its drug loading capacity（DL） and embedding ratio（ER） were 17.55% and 45.4% respectively.The release experiment in vitro drug showed that 5-FU was sustained-release effect from carboxymethylated chitosan microparticles with a cumulative amount of 94.92% after ten days.【Conclusion】 The carboxymethylated chitosan microparticle as a delivery system for 5-FU can change the pharmacokinetics properties of 5-FU by controlling its sustained-release effect and extending its cycling time,which may contribute to better anti-tumor effects of 5-FU in vivo.
出处
《中国现代医学杂志》
CAS
CSCD
北大核心
2011年第21期2584-2587,共4页
China Journal of Modern Medicine
基金
中国科学院西部之光项目(No.2005-24)
关键词
微粒
5-氟尿嘧啶
羧甲基壳聚糖
microparticle
5-fluorouraci
carboxymethylated chitosan
