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采用响应面法对表没食子儿茶素-3-没食子酸酯(EGCG)纳米脂质体条件进行优化及在Caco-2细胞中的细胞摄取研究

Optimization on condition of epigallocatechin-3-gallate (EGCG) nanoliposomes by response surface methodology and cellular uptake studies in Caco-2 cells.

作者信息

Luo Xiaobo, Guan Rongfa, Chen Xiaoqiang, Tao Miao, Ma Jieqing, Zhao Jin

机构信息

Zhejiang Provincial Engineering Laboratory of Quality Controlling Technology and Instrumentation for Marine Food, China Jiliang University, XueYuan Road 258#, 310018 Hangzhou, People's Republic of China.

Hubei Collaborative Innovation Center for Industrial Fermentation, Hubei University of Technology, Lizhi Road, 430068 Wuhan, China.

出版信息

Nanoscale Res Lett. 2014 Jun 10;9(1):291. doi: 10.1186/1556-276X-9-291. eCollection 2014.

Abstract

The major component in green tea polyphenols, epigallocatechin-3-gallate (EGCG), has been demonstrated to prevent carcinogenesis. To improve the effectiveness of EGCG, liposomes were used as a carrier in this study. Reverse-phase evaporation method besides response surface methodology is a simple, rapid, and beneficial approach for liposome preparation and optimization. The optimal preparation conditions were as follows: phosphatidylcholine-to-cholesterol ratio of 4.00, EGCG concentration of 4.88 mg/mL, Tween 80 concentration of 1.08 mg/mL, and rotary evaporation temperature of 34.51°C. Under these conditions, the experimental encapsulation efficiency and size of EGCG nanoliposomes were 85.79% ± 1.65% and 180 nm ± 4 nm, which were close with the predicted value. The malondialdehyde value and the release test in vitro indicated that the prepared EGCG nanoliposomes were stable and suitable for more widespread application. Furthermore, compared with free EGCG, encapsulation of EGCG enhanced its inhibitory effect on tumor cell viability at higher concentrations.

摘要

绿茶多酚的主要成分表没食子儿茶素没食子酸酯(EGCG)已被证明可预防癌症发生。为提高EGCG的有效性,本研究使用脂质体作为载体。除响应面法外,反相蒸发法是一种简单、快速且有益的脂质体制备和优化方法。最佳制备条件如下:磷脂酰胆碱与胆固醇的比例为4.00,EGCG浓度为4.88mg/mL,吐温80浓度为1.08mg/mL,旋转蒸发温度为34.51°C。在这些条件下,EGCG纳米脂质体的实验包封率和粒径分别为85.79%±1.65%和180nm±4nm,与预测值接近。丙二醛值和体外释放试验表明,所制备的EGCG纳米脂质体稳定,适合更广泛的应用。此外,与游离EGCG相比,EGCG的包封在较高浓度下增强了其对肿瘤细胞活力的抑制作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/612d/4059483/793cc7f1ce83/1556-276X-9-291-1.jpg

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