茶皂素作为生产橙皮苷纳米悬浮液的天然稳定剂。,International Journal of Pharmaceutics

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茶皂素作为生产橙皮苷纳米悬浮液的天然稳定剂。
International Journal of Pharmaceutics ( IF 5.3 ) Pub Date : 2020-05-05 , DOI: 10.1016/j.ijpharm.2020.119406
Jiaying Long ₁ , Jiawen Song ₁ , Xumin Zhang ₁ , Mao Deng ₁ , Long Xie ₁ , Linlin Zhang ₁ , Xiaofang Li ₁

Affiliation

茶皂素（TS），一种新型的多功能稳定剂，被研究来稳定纳米悬浮液。这项研究的目的是研究TS对纳米悬浮液的稳定性和可再分散性的影响。在目前的工作中，橙皮苷（HDN）是一种难溶药物，被用作模型药物。通过高速剪切和高压均质，制备了粒径为250-270 nm的HDN纳米悬浮液（HDN-NS）。HDN-NS的Zeta电位为-23.16±1.12 mV。与传统稳定剂相比，TS在低浓度下的稳定效率更高。用TS和乳糖作为冷冻保护剂的纳米悬浮液冻干粉具有良好的再分散性，重构后的平均粒径为266.5±9.0 nm。TS和乳糖可有效防止HDN-NS在冷冻干燥过程中发生不可逆的团聚。由于粒度减小，溶解度增加。透射电子显微镜（TEM）和扫描电子显微镜（SEM）的结果表明，HDN纳米晶体是不规则的块状。HDN的化学结构和晶体状态在生产过程中没有显着变化。总之，TS具有稳定和分散纳米悬浮液的潜力，并为难溶性药物的开发提供了有希望的策略。HDN的化学结构和晶体状态在生产过程中没有显着变化。总之，TS具有稳定和分散纳米悬浮液的潜力，并为难溶性药物的开发提供了有希望的策略。HDN的化学结构和晶体状态在生产过程中没有显着变化。总之，TS具有稳定和分散纳米悬浮液的潜力，并为难溶性药物的开发提供了有希望的策略。

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Tea saponins as natural stabilizers for the production of hesperidin nanosuspensions.

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.

更新日期：2020-05-05

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