School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610072, PR China.
School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610072, PR China.
Int J Pharm. 2020 Jun 15;583:119406. doi: 10.1016/j.ijpharm.2020.119406. Epub 2020 May 5.
Tea saponins (TS), a novel multifunctional stabilizer, were explored to stabilize the nanosuspensions. The purpose of this study was to investigate the effect of TS on the stability and redispersibility of nanosuspensions. In present work, hesperidin (HDN), a poorly soluble drug, was used as a model drug. HDN nanosuspensions (HDN-NS) with particle size of 250-270 nm were prepared by high-speed shearing and high-pressure homogenization. The zeta potential of HDN-NS was -23.16 ± 1.12 mV. Compared with traditional stabilizers, TS were superior in stabilization efficiency at low concentrations. Nanosuspensions freeze-dried powder using TS and lactose as cryoprotectants had good redispersibility, and the average particle size was 266.5 ± 9.0 nm after reconstitution. TS and lactose can effectively prevent the irreversible agglomeration of HDN-NS during freeze-drying. The dissolution was enhanced owing to particle size reduction. Transmission electron microscopy (TEM) and Scanning electron microscopy (SEM) results showed that HDN nanocrystals were irregularly lumpy. The chemical structure and crystal state of HDN had not significantly changed during production. In conclusion, TS have the potential to stabilize and disperse nanosuspensions and provide a promising strategy for the development of poorly soluble drugs.
茶皂素（TS）作为一种新型多功能稳定剂，被探索用于稳定纳米混悬剂。本研究旨在考察 TS 对纳米混悬剂稳定性和再分散性的影响。在本工作中，橙皮苷（HDN）作为一种难溶性药物被用作模型药物。通过高速剪切和高压匀质法制备粒径为 250-270nm 的 HDN 纳米混悬剂（HDN-NS）。HDN-NS 的 Zeta 电位为-23.16±1.12mV。与传统稳定剂相比，TS 在低浓度下具有更高的稳定效率。以 TS 和乳糖作为冻干保护剂的纳米混悬剂冻干粉末具有良好的再分散性，重悬后平均粒径为 266.5±9.0nm。TS 和乳糖可以有效地防止 HDN-NS 在冻干过程中的不可逆聚集。由于粒径减小，溶解得到增强。透射电子显微镜（TEM）和扫描电子显微镜（SEM）结果表明，HDN 纳米晶呈不规则块状。在生产过程中，HDN 的化学结构和晶体状态没有明显变化。总之，TS 有可能稳定和分散纳米混悬剂，并为开发难溶性药物提供了有前途的策略。
