摘要
以茶皂素(tea saponin, TS)为稳定剂,制备橙皮苷纳米混悬剂(hesperidin nanosuspensions, HDN-NS),考察TS作为新型天然稳定剂的可行性及其稳定纳米混悬剂的机制,为橙皮苷绿色纳米制剂的开发提供参考。以高速剪切联合高压均质法制备HDN-NS,以平均粒径及多分散指数为评价指标,采用单因素实验考察药物浓度、剪切速度、剪切时间、均质压力和均质次数对HDN-NS的影响。单因素实验考察结果为:药物浓度为8.0 mg·mL^(-1),剪切转速为16 000 r·min^(-1),剪切时间为2 min,在35 MPa下均质6次,再在100 MPa下均质12次。通过pH、离子强度、zeta电位和TS的临界胶束浓度等因素考察,确定静电斥力在TS稳定纳米混悬剂的机制中发挥的作用。稳定机制考察结果说明,静电斥力参与了TS稳定HDN-NS的机制。由此可知,低浓度下的TS可显著降低HDN-NS的粒径,表明TS具有稳定纳米混悬剂的潜力,静电作用是TS稳定纳米混悬剂的机制之一。
Hesperidin nanosuspensions(HDN-NS) were prepared with tea saponin(TS) as stabilizer. The feasibility of TS as a natural stabilizer and the mechanism of TS stabilized nanosuspensions were investigated to provide reference for the development of green nano-preparations of hesperidin. HDN-NS was prepared by highspeed shearing combined with high-pressure homogenization. Using average particle size and polydispersity index as evaluation indexes, the effects of drug concentration, shearing speed, shearing time, homogeneous pressure and homogeneous cycles on HDN-NS were investigated by single factor experiment. The results of single factor investigation were as follows: drug concentration was 8.0 mg·mL^(-1), shearing speed was 16 000 r·min^(-1), shearing time was 2 min, the homogeneous cycles were 6 cycles at 35 MPa and 12 cycles at 100 MPa. The pH, ionic strength,zeta potential and critical micelle concentration of TS were investigated to determine the role of electrostatic repulsion in the mechanism of TS stabilized nanosuspensions. The results showed that electrostatic repulsion is involved in the mechanism of TS stabilized HDN-NS. In conclusion, at low concentration, TS can significantly reduce the particle size of HDN-NS, which indicates that TS has the potential to stabilize nanosuspension. Electrostatic repulsion is one of the mechanisms of TS stabilizing nanosuspension.
作者
龙家英
李小芳
王娴
邓茂
古环
谢龙
陈慧娟
代小琳
LONG Jia-ying;LI Xiao-fang;WANG Xian;DENG Mao;GU Huan;XIE Long;CHEN Hui-juan;DAI Xiao-lin(The Ministry of Education Key Laboratory of Standardization of Chinese Herbal Medicine,State Key Laboratory of Characteristic Chinese Medicine Resources in Southwest China,Pharmacy College,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China)
出处
《药学学报》
CAS
CSCD
北大核心
2021年第11期3159-3165,共7页
Acta Pharmaceutica Sinica
基金
四川省科技创新苗子工程项目(2020095)
四川省科技厅重点项目(2019YFS0113)。
关键词
茶皂素
橙皮苷
纳米混悬剂
制备工艺
稳定机制
绿色纳米制剂
天然稳定剂
tea saponin
hesperidin
nanosuspension
preparation technology
stabilizing mechanism
green nano-preparation
natural stabilizer
