阿霉素纳米制剂的制备

Preparation of doxorubicin nanoparticles

为了制备具有增加药物溶解度、提高药物生物利用度、增强抗肿瘤效果的新制剂,试验以明胶-环糊精聚合物为载体、阿霉素为药物制备阿霉素纳米制剂,并对其性质进行考察。采用Zetasizer Nano激光粒度测定仪测定阿霉素纳米制剂的粒径、多分散性指数(PDI)和Zeta电位,HPLC法测定其包封率,重量法测定纳米制剂载药量,透射电镜法观察纳米制剂形态,透析法测定纳米制剂的体外释放行为。结果表明:明胶-环糊精聚合物与药物比例10∶1、室温搅拌6 h、探头超声10 min条件下制备的纳米制剂粒径较小且粒径大小最均一,其粒径为(148.60±4.20)nm,PDI为0.13±0.01,Zeta电位为(-2.68±0.03)mV,包封率为(98.66±0.07)%,载药量为(8.98±0.04)%,纳米制剂形态为球形,且大小较为均匀。说明该制剂具有明显缓释效果,具有良好的性质。

In order to prepare a new preparation with drug solubility,drug bioavailability and anti-tumor effect,doxorubicin nanoparticles were prepared with Gelatin Graftedβ-Cyclodextrin as the carrier and doxorubicin as the drug,and their properties were investigated.The particle size,polydispersability index(PDI)and Zeta potential of doxorubicin nanoparticles were measured by Zetasizer nano laser particle size analyzer.The encapsulation efficiency was tested by HPLC,and drug loading of doxorubicin nanoparticle was measured by gravimetric analysis.The morphology of the nanoparticles was observed by transmission electron microscopy,and the release behavior of the nanoparticles in vitro was determined by dialysis method.The results showed that the ratio of carrier polymer to drug was 10∶1,the nanoparticles were prepared under the conditions of stirring at room temperature for 6 h and ultrasonic probe for 10 min with small particle size and the most uniform particle size.The doxorubicin nanoparticle was(148.60±4.20)nm,PDI was 0.13±0.01 and Zeta potential was(-2.68±0.03)mV.The encapsulation efficiency was(98.66±0.07)%,and the drug loading was(8.98±0.04)%.The images of the nanoparticle was spherical shape and had a narrow size distribution.It indicated that doxorubicin nanoparticles showed a sustained release profile,and it had good properties,which provided an important guarantee for the clinical application of drug preparation in tumor diseases.