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目的制备透明质酸修饰的白蛋白纳米粒,对其修饰程度和载药性能进行考察,并初步评价其抗肿瘤作用。方法用去溶剂化法制备白蛋白纳米粒,并用透明质酸修饰纳米粒表面,以表面活性氨基的减少作为评价透明质酸修饰的白蛋白纳米粒的修饰程度的指标,并筛选最佳处方;考察pH和载药量及包封率的关系。使用噻唑蓝比色法(MTT)测定纳米粒对人肝癌细胞株HepG2的抑制率。结果制备所得的透明质酸修饰的白蛋白纳米粒的平均粒径为396 nm,Zeta电位-19.7 mV,表面氨基减少率为34.28%;透明质酸修饰的米托蒽醌白蛋白纳米粒载药量11.13%,包封率94.64%,平均粒径为398 nm,Zeta电位-17.9 mV,且具有明显的缓释作用。透明质酸修饰的米托蒽醌白蛋白纳米粒比米托蒽醌水溶液具有更强的细胞抑制率(P<0.05)。结论所用制备工艺稳定,可用于制备透明质酸修饰的白蛋白纳米粒。透明质酸修饰的米托蒽醌白蛋白纳米粒具有不低于药物溶液的活性。
Objective To prepare hyaluronic acid-modified albumin nanoparticles and investigate the degree of modification and drug-loading properties of the nanoparticles. The anti-tumor effects of hyaluronic acid nanoparticles were evaluated. Methods The albumin nanoparticles were prepared by desolvation method. The surface of nanoparticles was modified by hyaluronic acid. The reduction of surface amino groups was used as an index to evaluate the degree of modification of hyaluronic acid - modified albumin nanoparticles and the best prescription was selected. The relationship between pH and drug loading and entrapment efficiency was investigated. The inhibitory rate of nanoparticles on human hepatocellular carcinoma cell line HepG2 was determined by MTT assay. Results The average particle size of the prepared hyaluronic acid-modified albumin nanoparticles was 396 nm, the Zeta potential was -19.7 mV, and the surface amino group reduction rate was 34.28%. The hyaluronic acid-modified mitoxantrone albumin nanoparticles Amount of 11.13%, encapsulation efficiency of 94.64%, the average particle size of 398 nm, Zeta potential of -17.9 mV, and has a significant sustained-release effect. Hyaluronic acid-modified mitoxantrone albumin nanoparticles had a stronger cytostatic rate than mitoxantrone aqueous solution (P <0.05). Conclusion The preparation process is stable and can be used to prepare hyaluronic acid modified albumin nanoparticles. Hyaluronic acid-modified mitoxantrone albumin nanoparticles have no less than drug solution activity.