表面活性剂对高水溶性药物阿魏酸钠白蛋白纳米粒的载药特性影响

目的:制备高水溶性药物白蛋白纳米粒,考察表面活性剂对高水溶性药物的包封作用。方法:以牛血清白蛋白为载体材料,阿魏酸钠为高水溶性药物模型,采用去溶剂化法制备阿魏酸钠白蛋白纳米粒。用低温超速离心法、层析-离心法、层析-酶解法对纳米粒包封率和载药量进行测定评价,并考察表面活性剂对纳米粒包封率、载药量及得率的影响。结果和结论:层析-离心法测定结果可靠。亲水性表面活性剂0.3%洛泊沙姆和亲脂性表面活性剂0·48%卵磷脂联合使用,有利于高水溶性药物的包封,包封率为28.42%,载药量为10.5%。

Effects of surfactants on the pharmaceutical characteristics of bovine serum albumin nanoparticles of highly water-soluble drug sodium ferulate

Objective: To prepare the highly water-soluble drug (HWS-drug) bovine serum albumin nanoparticles, and study the effects of surfactants on them. Methods: Sodium ferulate bovine serum albumin nanoparticles (SF-BSA-NP) were prepared from sodium ferulate (SF), which was a HWS-drug, and bovine serum albumin (BSA) by desolvation method. Using the methods of ultracentrifugation, chromatography-ultracentrifugation and chromatography-trypsin degradation, the entrapment efficiency and drug loading of SF-BSA-NP were determined, respectively. The effects of surfactants on the entrapment efficiency and drug loading were studied. Results and Conclusion: The entrapment efficiency and drug loading measured by the method of chromatography-ultracentrifugation were reliable. Hydrophilic surfactant together with lipophilic surfactant could benefit the preparation of HWS-drug bovine serum albumin nanoparticles. The entrapment efficiency was 28.42% and drug loading was 10.5%.