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含功能性稳定剂的纳米颗粒药物悬浮液的冷冻干燥用抗冻剂选择和分析。

Cryoprotectant choice and analyses of freeze-drying drug suspension of nanoparticles with functional stabilisers.

机构信息

a School of Chemistry and Pharmaceutical Engineering , Qilu University of Technology (Shandong Academy of Sciences) , Jinan , PR China.

出版信息

J Microencapsul. 2018 May;35(3):241-248. doi: 10.1080/02652048.2018.1462416. Epub 2018 Apr 19.

Abstract

Freeze-drying is an effective way to improve long-term physical stability of nanosuspension in drug delivery applications. Nanosuspension also known as suspension of nanoparticles. In this study, the effect of freeze-drying with different cryoprotectants on the physicochemical characteristics of resveratrol (RSV) nanosuspension and quercetin (QUE) nanosuspension was evaluated. D-α-tocopheryl polyethylene glycol succinate (TPGS) and folate-modified distearoylphosphatidyl ethanolamine-polyethylene glycol (DSPE-PEG-FA) were selected as functional stabilisers formulated nanosuspension which were prepared by anti-solvent precipitation method. RSV nanoparticle size and QUE nanoparticle size were about 210 and 110 nm, respectively. The AFM and TEM results of nanosuspension showed uniform and irregular shape particles. After freeze-drying, the optimal concentration of four cryoprotectants was determined by the particle size of re-dispersed nanoparticles. The dissolution profile of drug nanoparticle significantly showed approximately at a 6-8-fold increase dissolution rate. Moreover, TPGS and DSPE-PEG-FA stabilised RSV nanosuspension and QUE nanosuspension samples showed better effect on long-term physical stability.

摘要

冷冻干燥是提高药物递送应用中纳米混悬剂长期物理稳定性的有效方法。纳米混悬剂也称为纳米颗粒混悬剂。在这项研究中,评估了不同冷冻保护剂对白藜芦醇(RSV)纳米混悬剂和槲皮素(QUE)纳米混悬剂物理化学特性的影响。选择 D-α-生育酚聚乙二醇琥珀酸酯(TPGS)和叶酸修饰的二硬脂酰基磷脂酰乙醇胺-聚乙二醇(DSPE-PEG-FA)作为功能性稳定剂,通过抗溶剂沉淀法制备纳米混悬剂。RSV 纳米颗粒粒径和 QUE 纳米颗粒粒径分别约为 210nm 和 110nm。纳米混悬剂的 AFM 和 TEM 结果表明其为均匀和不规则形状的颗粒。冷冻干燥后,通过再分散纳米颗粒的粒径确定了四种冷冻保护剂的最佳浓度。药物纳米颗粒的溶解曲线显示出约 6-8 倍的溶解速率显著增加。此外,TPGS 和 DSPE-PEG-FA 稳定的 RSV 纳米混悬剂和 QUE 纳米混悬剂样品对长期物理稳定性具有更好的效果。

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