摘要
本试验使用生物表面活性剂酸型槐糖脂(ASL)替代Tween-80为表面活性剂制备了一种新型依托泊苷纳米乳注射剂(ENE),并通过比较含ASL或Tween-80纳米乳的理化性质及稳定性,考察用ASL替代Tween-80的可行性。采用高压均质法制备纳米乳注射剂,所得ASL-ENE和Tween-ENE的粒径为(206.7±0.1)和(204.6±0.2)nm,ζ电位为(-38.4±0.2)和(-45.1±0.1)mV,包封率为(96.40±0.45)%和(97.07±0.09)%。并且,考察了初乳pH值和灭菌方式对纳米乳质量的影响。结果表明,高压均质前将初乳调至pH 5.55,所得ASL-ENE在80℃下的药物半衰期为32.84 h,121℃高压蒸汽灭菌20min前后的粒径及ζ电位均无明显变化。4℃保存3个月的稳定性试验和溶血试验结果显示,ASL-ENE的物理稳定性优于Tween-ENE,且未发生溶血现象。上述结果说明用生物表面活性剂ASL替代常用化学表面活性剂Tween-80制备依托泊苷纳米乳是可行的。
To investigate the feasibility of using acidic sophorolipid(ASL), a novel biosurfactant, instead of Tween-80 for the preparation of etoposide nanoemulsion(ENE), two types of ENE for injection were prepared by high-pressure homogenization, and their stabilities as well as hemolysis were compared. The results showed that the average particle size, ζ potential and entrapment efficiency for ASL-ENE were(206.7±0.1)nm,(-38.4±0.2)mV and(96.40±0.45)%, while for Tween-ENE were(204.6±0.2)nm,(-45.1±0.1)mV and(97.07±0.09)%. The effects of pH value of crude emulsion and sterilization method on the quality of ENEs were also investigated. The results showed that the half-life period of etoposide in ASL-ENE at 80 ℃ was prolonged to 32.84 h when the pH value of crude emulsion was adjusted to 5.55. Moreover, there were no significant differences for ASL-ENE before and after steam sterilization at 121 ℃for 20 min in average particle size and ζ potential values. The ASL-ENE exhibited superior stability to the Tween-ENE in a long-term stability test at 4 ℃ for 3 months. Furthermore, ASL-ENE showed less hemolysis and higher safety than Tween-ENE. These results demonstrated that it was feasible to prepare ENE with this biosurfactant ASL instead of the chemical surfactant Tween-80.
作者
马晓静
孟莉
余子安
于泽权
何天义
MA Xiaojing;MENG Li;YU Zian;YU Zequan;HE Tianyi(Anhui Nature Pharmaceutical Co.,Ltd.,Yue Kang Pharmaceutical Group,Fuyang 236033;School of Food and Biological Engineering,Hefei University of Technology,Hefei 230009)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2020年第2期226-232,共7页
Chinese Journal of Pharmaceuticals
基金
中央高校基本科研业务费专项资金项目(JZ2019YYPY0029)
国家自然科学基金青年基金(31400049)。
