重组人白介素-2壳聚糖鼻腔黏附微球的制备、评价及对家兔过敏性鼻炎的药效研究  

Preparation,Characterization of Nasal Mucoadhesive Microspheres of Recombinant Human Interleukin-2 Based on Chitosan and Their Effect on Allergic Rhinitis in Rabbits

作　　者：汤玥[1] 任海霞[1] 姜力群[1] 程度胜 朱家壁[1] 

机构地区：[1]中国药科大学药学院,南京210009 [2]北京四环生物制药有限公司,北京100176

出　　处：《中国药学杂志》2010年第17期1335-1339,共5页Chinese Pharmaceutical Journal

基　　金："重大新药创制"科技重大专项(2009ZX09310-004)

摘　　要：目的制备重组人白介素-2(rhIL-2)壳聚糖鼻腔黏附微球。并评价其用于过敏性鼻炎的可能性。方法采用沉淀方法制备载药微球,并对其外观形态、粒径、Zeta电位、载药量以及体外释放行为进行考察。结果以相对分子质量较大的壳聚糖制备的微球具有较大的粒径。体外释放实验表明,rhIL-2壳聚糖微球具有一定的缓释效果。黏膜纤毛迁移速率实验显示壳聚糖微球具有黏膜黏附性。家兔过敏性鼻炎实验表明,鼻腔给予该制剂可以缓解过敏性鼻炎症状,减少打喷嚏的发生率并且降低血浆中NO的含量。结论 rhIL-2壳聚糖微球比相同剂量rhIL-2溶液具有更好的效果。OBJECTIVE To develop nasal mucoadhesive microspheres of recombinant human interleukin-2（rhIL-2） based on chitosan.METHODS The microspheres were prepared using the precipitation technique and characterized in terms of particle morphology,particle size,Zeta potential,drug loading and in vitro drug release.RESULTS The chitosan with higher molecular weight formed microspheres with larger particle size.In vitro release studies showed that rhIL-2-loaded microspheres provided sustained release effect.The mucociliary transport rate（MTR） studies suggested that chitosan microspheres had mucoadhesive characteristics.The experiments of allergic rhinitis in rabbits showed that rhIL-2 alleviated allergic rhinitis symptoms after nasal administration,decreased the occurrence of sneezing and the content of nitric oxide in the serum.CONCLUSION At the same dose,the effect of rhIL-2 chitosan microsphere was better than that of solution.

关 键 词：重组人白介素-2 鼻腔黏附性微球 壳聚糖 过敏性鼻炎 

分 类 号：R944[医药卫生—药剂学]