半乳糖化白蛋白磁性阿霉素纳米粒制备工艺的优化及缓释性的研究

Preparation of galactosyl-HSA-magnetic-adriamycin-nanoparticles and study of their physical property

目的 制备具有稳定磁性、能够携带化疗药物的半乳糖化白蛋白磁性纳米粒,并对纳米粒的磁性、药物含量、包封率、粒径大小等物理性质进行检测。方法 运用正交试验设计方法设计实验,以粒径大小、纳米药物的载药量和包封率3个指标考察固化温度、固化时间、搅拌速度及糖化比率4个因素的4个水平,从中选出最优化组合,并以最优化组合重复实验,验证试验条件的稳定性以及实验的可重复性。先行制备半乳糖化白蛋白,将阿霉素、半乳糖化白蛋白、磁粉按一定比例混合,通过在精制棉籽油中超声乳化、加热变性固化、乙醚洗涤等工艺制作出载药纳米粒,用乙醇提取法提取纳米粒中的阿霉素,并用紫外分光光度计测定含量,激光粒度分析仪分析粒径大小。结果 运用最优化条件制备的纳米粒,其平均粒径为(197±32)mm,载药量(48.79±4.47)mg/L,包封率(94.34±3.32)％。结论 上述优化条件稳定,试验的可重复性高。

Objective To prepare galactosyl-HSA-magnetic-adriamycin-nanopartides (ADR-GHMN), measure physical properties of the ADR-GHNM, such as magnetism, galactose density (GD), drug loading (DL) and size of manoparticles. Methods By using the method of orthogonal design, through evaluating the nanoparticles from DL, size of nanoparticles and trap efficiency, effects of solidification temperature, solidification time, mix speed and galactose density were observed on the 4 levels in the course of preparing ADR-GHMN, respectively. From the 4 levels, the best one was chosen, and the experiment was repeated to verify repeatability and stabilities of this experimental condition. Galactosyl-HAS was prepared firstly, then mixed with adriamycin and magnetites poweder according to appropriate proportion. Then the nanoparticles were produced by sonication in cottonseed oil, heat polymerization and washing with aether, Results The average size of the nanoparticles prepared by the above method was (197±32) nm, drug loading was (48.79±4.47) mg/L, trap efficiency was (94.34±3.32)%. Conclusion Above mentioned optimal condition was stable and the repeatability of the experiment was satisfactory.