重组人血管内皮抑素壳聚糖纳米粒的制备及体外评价

采用离子凝胶法制备重组人血管内皮抑素(商品名:Endostar)壳聚糖纳米粒,并对纳米粒的载药量、包封率、粒径、形态、体外释放、体外活性及Endostar结构的完整性进行考察。制得的Endostar壳聚糖纳米粒载药量为(10.5±1.1)%,包封率为(81.3±1.8)%;平均粒径为137 nm,为球形结构;体外释放10 d累积释放达到80%。凝胶电泳实验说明Endostar结构完整,制备与释放过程结构均未被破坏;人脐静脉内皮细胞增殖实验说明Endostar纳米粒仍保留原有的生物活性。结果表明壳聚糖作Endostar的载体,制得的纳米粒具有合适的粒径及包封率,并能达到缓释作用,不会破坏Endostar的结构,同时保留原有的生物活性。

Preparation and in vitro evaluation of chitosan nanoparticles encapsulating recombinant human endostatin

Chitosan nanoparticles encapsulating recombinant human endostatin (Endostar) were prepared by the ionic gelation process.Characterizations including drug loading,encapsulation efficiency,particle size,morphology,in vitro release,bioactivity and the integrity of Endostar were investigated.It was found that drug loading and encapsulation efficiency were (10.5±1.1)% and (81.3±1.8)%,respectively.The average particle diameter of the spheric nanoparticles was 137 nm.80% of cumulative release was achieved after 10 d.The results of SDS-PAGE indicated no change to the structure of Endostar during the process of preparation and in vitro release.The endothelial cell proliferation assay showed that the nanoparticles retained the bioactivity of the protein.These results indicated that Endostar nanoparticles prepared with chitosan possessed appropriate particle size and encapsulation efficiency,exhibited sustained release in vitro,maintained the structure of Endostar,and retained the bioactivity of the protein.