摘要
探索绞股蓝皂苷作为一种新型天然稳定剂生产纳米混悬剂的潜力。以槲皮素为模型药,通过高速剪切-高压均质法制备绞股蓝皂苷稳定的槲皮素纳米混悬剂(quercetin nanosuspensions, QUE-NS),并对其进行体外评价。基于QUE-NS平均粒径和多分散指数(polydispersity index, PDI)的测定结果,采用单因素试验优化制备工艺参数。通过冷冻干燥法将QUE-NS制备成冻干粉,并进行储存稳定性和饱和溶解度研究。此外,还考察了pH和离子强度对纳米混悬液体系物理稳定性的影响。结果表明,优化的工艺参数为剪切转速13 000 r·min^(-1)、剪切时间2 min、均质压力100 MPa、均质次数12次,在此条件下制备的QUE-NS平均粒径为(461.9±2.4)nm, PDI为0.059±0.016。在室温下储存2个月期间,QUE-NS冻干粉保持稳定。饱和溶解度结果表明QUE-NS冻干粉的饱和溶解度高于槲皮素原料药和物理混合物。稳定性测试结果显示绞股蓝皂苷稳定的纳米混悬液在pH 6~8表现出良好的稳定性,而在盐存在的条件下容易发生聚集。总之,绞股蓝皂苷有望成为一种新型的天然稳定剂用于纳米混悬剂的制备。
This study was designed to explore the potential of gypenosides as a novel natural stabilizer for the production of nanosuspensions. The gypenosides-stabilized quercetin nanosuspensions(QUE-NS) were prepared using the high-speed shearing and high-pressure homogenization method with quercetin as a model drug, followed by their in vitro evaluation.Based on the measured mean particle size and polydispersity index(PDI) of QUE-NS,the single factor experiment was conducted to optimize the preparation process parameters.The freeze-drying method was used to transform QUE-NS into freeze-dried powders, whose storage stability and saturation solubility were then studied.Moreover, the effects of pH and ionic strength on the physical stability of the nanosuspension system were examined.According to the results, the optimized process parameters were listed as follows: shear rate 13 000 r·min^(-1),shear time 2 min, homogenization pressure 100 MPa, and homogenization frequency 12 times.The mean particle size of QUE-NS prepared under the optimum process conditions was(461.9±2.4) nm, and the PDI was 0.059±0.016.During the two months of storage at room temperature, the freeze-dried QUE-NS powders remained stable.The saturation solubility of freeze-dried QUE-NS powders was proved higher than those of quercetin and the physical mixture.The results of stability testing demonstrated that QUE-NS stabilized with gypenosides exhibited good stability within the pH range of 6 to 8,while coalescence was prone to occur in the presence of salt.Overall, gypenosides is expected to become a new natural stabilizer for the preparation of nanosuspensions.
作者
陈慧娟
李小芳
邓茂
谢龙
刘凯
张旭敏
CHEN Hui-juan;LI Xiao-fang;DENG Mao;XIE Long;LIU Kai;ZHANG Xu-min(School of Pharmacy,Chengdu Universily of Traditional Chinese Medicine,Chengdu 611137,China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2022年第16期4365-4371,共7页
China Journal of Chinese Materia Medica
基金
四川省科技厅项目(2019YFS0113)。
