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目的以壳聚糖(CS)为载体,研究其对重组人血管内皮抑制素(Endostar)的包封及控释能力。方法采用大分子复合法制备纳米粒,考察形成条件及冻干工艺,并对纳米粒的形态、包封率、体外释放及Endostar的完整性进行考察。结果 CS与羧甲基纤维素钠(CMC-Na)的质量比介于6∶1～1∶2时可以形成纳米粒,粒径为142～176 nm。壳聚糖分子量的增加可使粒径和包封率均增加;理论载药量由10%增至30%时,粒径增加,但包封率先增加后降低。以外观和复溶后的粒径作为评价指标筛选海藻糖为适宜的冻干保护剂。冻干后的纳米粒为球形结构,10 d的累积释放达70%。凝胶电泳(SDS-PAGE)结果表明了Endostar结构完整,制备及释放过程中结构未被破坏。结论壳聚糖作为Endostar的载体所制备的纳米粒具有合适的粒径及包封率,并能达到缓释作用,且不会破坏Endostar的结构。
Objective Chitosan (CS) was used as a carrier to study the encapsulation and release of recombinant human endostar. Methods Nanoparticles were prepared by macromolecule complex method. The formation conditions and freeze-drying process were investigated. The morphology, entrapment efficiency, release in vitro and the integrity of Endostar were investigated. Results The mass ratio of CS to CMC-Na ranged from 6: 1 to 1: 2. The increase of molecular weight of chitosan can increase the particle size and entrapment efficiency. When the theoretical drug loading increased from 10% to 30%, the particle size increased, but the entrapment efficiency increased firstly and then decreased. The appearance and the particle size after reconstitution were used as the evaluation index to select trehalose as suitable lyoprotectant. The lyophilized nanoparticles were spherical in shape, with a cumulative release of 70% after 10 days. SDS-PAGE showed that the structure of Endostar was intact and its structure was not damaged during preparation and release. Conclusion The nanoparticles prepared by chitosan as a carrier of Endostar have suitable particle size and entrapment efficiency, and can achieve sustained release without damaging the structure of Endostar.