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喷雾干燥法制备高抗氧化活性保留的单分散表没食子儿茶素没食子酸酯(EGCG)微球。

Production of monodisperse epigallocatechin gallate (EGCG) microparticles by spray drying for high antioxidant activity retention.

机构信息

Department of Chemical Engineering, Monash University, Clayton, Victoria 3800, Australia.

出版信息

Int J Pharm. 2011 Jul 15;413(1-2):155-66. doi: 10.1016/j.ijpharm.2011.04.056. Epub 2011 Apr 28.

Abstract

Epigallocatechin gallate (EGCG) originated from green tea is well-known for its pharmaceutical potential and antiproliferating effect on carcinoma cells. For drug delivery, EGCG in a micro-/nanoparticle form is desirable for their optimized chemopreventive effect. In this study, first time reports that EGCG microparticles produced by low temperature spray drying can maintain high antioxidant activity. A monodisperse droplet generation system was used to realize the production of EGCG microparticles. EGCG microparticles were obtained with narrow size distribution and diameter of 30.24 ± 1.88 μM and 43.39 ± 0.69 μM for pure EGCG and lactose-added EGCG, respectively. The EC50 value (the amount of EGCG necessary to scavenge 50% of free radical in the medium) of spray dried pure EGCG particles obtained from different temperature is in the range of 3.029-3.075 μM compared to untreated EGCG with EC50 value of 3.028 μM. Varying the drying temperatures from 70°C and 130°C showed little detrimental effect on EGCG antioxidant activity. NMR spectrum demonstrated the EGCG did not undergo chemical structural change after spray drying. The major protective mechanism was considered to be: (1) the use of low temperature and (2) the heat loss from water evaporation that kept the particle temperature at low level. With further drier optimization, this monodisperse spray drying technique can be used as an efficient and economic approach to produce EGCG micro-/nanoparticles.

摘要

表没食子儿茶素没食子酸酯(EGCG)源于绿茶,以其药用潜力和对癌细胞的抗增殖作用而闻名。对于药物输送,以微粒/纳米颗粒形式存在的 EGCG 因其优化的化学预防作用而受到青睐。在这项研究中,首次报道了由低温喷雾干燥产生的 EGCG 微粒可以保持高抗氧化活性。使用单分散液滴生成系统来实现 EGCG 微粒的生产。分别获得了粒径分布窄且直径为 30.24 ± 1.88 μM 和 43.39 ± 0.69 μM 的纯 EGCG 和添加乳糖的 EGCG 微粒。与未经处理的 EGCG 的 EC50 值(清除培养基中 50%自由基所需的 EGCG 量)相比,不同温度下获得的喷雾干燥纯 EGCG 颗粒的 EC50 值在 3.029-3.075 μM 范围内。将干燥温度从 70°C 和 130°C 变化对 EGCG 抗氧化活性几乎没有不利影响。NMR 谱表明 EGCG 在喷雾干燥后没有发生化学结构变化。主要的保护机制被认为是:(1)使用低温和(2)水蒸发的热损失使颗粒温度保持在低温水平。通过进一步的干燥优化,这种单分散喷雾干燥技术可作为一种高效、经济的方法来生产 EGCG 微/纳米颗粒。

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