重组水蛭素-2鼻腔黏附纳米粒的体外评价

Evaluation of nasal mucoadhesive nanoparticles of recombinate hirudin-2 in vitro

目的:对制备的重组水蛭素-2(rHV2)壳聚糖鼻腔黏附纳米粒进行体外评价。方法:测定纳米粒的形态、粒径大小分布及表面电位;以超速离心测定纳米粒在不同介质中的释放度;采用在体蟾蜍上腭纤毛运动试验法考察纳米粒的纤毛毒性。结果:制备的rHV2壳聚糖纳米粒呈较为均匀分散的颗粒状,平均粒径为213.2 nm,纳米粒带正电荷,Zeta电位值为+30.61 mV,体系相对稳定性较高;rHV2纳米粒在乙酸缓冲液中的累积释放百分数明显高于在磷酸缓冲液中的累积释放百分数;rHV2纳米粒溶液的纤毛毒性较小(与生理盐水组相比,P>0.05)。结论:壳聚糖鼻腔黏附纳米粒有望成为rHV2鼻腔给药的递释系统。

Objective：To evaluate the properties of rHV2 chitosan mucoadhesive nanoparticle for nasal de- livery in vitro. Methods ： The physicochemical properties of the nanoparticles, such as morphological characters, par- ticle sizedistribution and Zeta potential were examined,and the release rate of rHV2 from chitosan nanoparticles in different medium was determined by ultracentrifugation;the ciliotoxicity of rHV2 nanoparticles was also evaluated with in situ toad palate ciliary movement experiment. Results：rHV2 nanoparticles with even particle size distribu- tion were prepared. The average particle diameter was 213.2 nm, and the particles were positive with 30.61 mV Zeta potential. The accumulated release percentage of rHV2 from nanoparticle~ in acetate buffer was higher than in PBS ;the ciliotoxicity of rHV2 nanopartieles solution was not stronger than saline （ P 〉 0.05 ）. Conclusion ： Chi- tosan mucoadhesive nanoparticles are supposed to be a better delivery system for rHV2 nasal administration.