藤黄酸白蛋白纳米粒的构建及体外抗肿瘤治疗

Albumin Nanoparticles Loading Gambogic Acid for Cancer Therapy in Vitro

目的构建藤黄酸白蛋白纳米粒,提升藤黄酸的药物特性。方法通过溶剂置换法制备纳米粒,将藤黄酸甲醇溶液逐滴加入到牛血清白蛋白水溶液中,以牛血清白蛋白偶联中药藤黄酸,再用戊二醛交联保持其稳定性。通过粒径分布、透射电镜、Zeta电位等方法对纳米粒进行表征,并利用紫外可见光分光光度计测定其载药量与药物释放情况。结果当牛血清白蛋白的质量浓度为4 mg·mL^(-1)时,制得的纳米粒稳定性良好,载药量高达79%。体外释放实验结果表明,纳米粒具有缓慢释药的特性。体外细胞抗肿瘤结果表明,将藤黄酸制备成纳米药物并不影响其药物特性。结论利用白蛋白纳米粒负载水不溶性中药,不仅能保留高载药量的优势,还可显著增强其稳定性,达到药物长效释放的目标。

Objective To construct gambogic acid-loaded albumin nanoparticles for improving the drug properties of gambogic acid.Methods The nanoparticles were prepared by solvent displacement method,and the gambogic acid-methanol solution was added to the aqueous bovine serum albumin solution.The gambogic acid was coupled with bovine serum albumin,and glutaraldehyde was then added to maintain the stability of the nanoparticles.Size distribution measurement,transmission electron microscopy and Zeta potential detection were performed to characterize the nanoparticles.Drug loading and release were determined using UV-Vis spectrophotometer.Results When the concentration of bovine serum albumin was 4 mg·mL^(-1),the nanoparticles prepared had good stability with a drug loading capacity of 79%.The result of in vitro release test showed that the nanoparticles had the characteristics of sluggish drug release.The result of in vitro antitumor test demonstrated that the pharmacological properties of gambogic acid were unaffected by the process used to prepared the nanoparticles.Conclusion The use of water-insoluble Chinese medicine loaded by albumin nanoparticles not only maintains the high drug loading capacity,but also improves the stability to accomplish the long-lasting drug release.