Chen Hui-Juan, Li Xiao-Fang, Deng Mao, Xie Long, Liu Kai, Zhang Xu-Min
School of Pharmacy, Chengdu University of Traditional Chinese Medicine Chengdu 611137, China.
Zhongguo Zhong Yao Za Zhi. 2022 Aug;47(16):4365-4371. doi: 10.19540/j.cnki.cjcmm.20210928.301.
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.
本研究旨在探索绞股蓝皂苷作为一种新型天然稳定剂用于制备纳米混悬液的潜力。以槲皮素为模型药物，采用高速剪切和高压均质法制备了绞股蓝皂苷稳定的槲皮素纳米混悬液（QUE-NS），随后对其进行体外评价。基于所测得的QUE-NS的平均粒径和多分散指数（PDI），进行单因素实验以优化制备工艺参数。采用冷冻干燥法将QUE-NS转化为冻干粉，然后研究其储存稳定性和饱和溶解度。此外，考察了pH值和离子强度对纳米混悬液体系物理稳定性的影响。根据结果，优化后的工艺参数如下：剪切速率13000 r·min⁻¹、剪切时间2 min、均质压力100 MPa、均质次数12次。在最佳工艺条件下制备的QUE-NS的平均粒径为（461.9±2.4）nm，PDI为0.059±0.016。在室温储存的两个月期间，冻干粉状的QUE-NS保持稳定。结果表明，冻干QUE-NS粉末的饱和溶解度高于槲皮素和物理混合物。稳定性测试结果表明，用绞股蓝皂苷稳定的QUE-NS在pH值6至8范围内表现出良好的稳定性，而在有盐存在的情况下容易发生聚结。总体而言，绞股蓝皂苷有望成为制备纳米混悬液的新型天然稳定剂。
