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壳聚糖纳米粒中同时载入(-)-表没食子儿茶素没食子酸酯和阿魏酸作为有效的抗氧化剂和潜在的皮肤增白剂。

Simultaneous loading of (-)-epigallocatechin gallate and ferulic acid in chitosan-based nanoparticles as effective antioxidant and potential skin-whitening agents.

机构信息

Department of Food Science and Engineering, Jinan University, Guangzhou 510632, China; Guangdong Joint International Research Centre of Oilseed Biorefinery, Nutrition and Safety, Jinan University, Guangdong Engineering Technology Research Center for Cereal and Oil Byproduct Biorefinery, Guangzhou 510632, China.

School of Science, Monash University Malaysia, 47500 Bandar Sunway, Selangor, Malaysia.

出版信息

Int J Biol Macromol. 2022 Oct 31;219:333-345. doi: 10.1016/j.ijbiomac.2022.07.242. Epub 2022 Aug 4.

Abstract

Chitosan (CS) based nanoparticles simultaneously loaded with (-)-epigallocatechin gallate (EGCG) and ferulic acid (FA) were fabricated via ionic gelation method modified by sodium tripolyphosphate and genipin (G-CS-EGCG-FA NPs). The particle size, morphology, entrapment efficiency, rheological properties, antioxidant and tyrosinase inhibitory activity of NPs were investigated. The G-CS-EGCG-FA NPs exhibited irregular ellipsoidal shape with average diameter of 412.3 nm and high DPPH and ABTS· scavenging ability. The entrapment efficiency of EGCG and FA in NPs was 46.0 ± 1.3 % and 46.8 ± 1.6 %, respectively. CS-based NPs show no toxic effects on NIH 3 T3 cells and B16-F10 melanoma cells with concentration <200 μg/mL and 25 μg/mL, respectively and the cell viability ranged from 100 % to 118 %. Meanwhile, the oxidative repaired capacity of G-CS-EGCG-FA NPs (200 μg/mL) in HO-induced cells was over 100 %, higher than that of the same dose of free EGCG or FA. Moreover, the tyrosinase inhibition activity of G-CS-EGCG-FA NPs (25 μg/mL) (84.6 %) was more potent than that of free EGCG (55.3 %), free FA (47.1 %) and kojic acid, indicating the good skin repairing and whitening ability of G-CS-EGCG-FA NPs. Given these results, this research provides new insights for designing novel particles loaded with dual bioactive agents that possess synergistic benefits.

摘要

壳聚糖(CS)基纳米粒子同时负载(-)-表没食子儿茶素没食子酸酯(EGCG)和阿魏酸(FA),通过离子凝胶法制备,并用三聚磷酸钠和京尼平(G-CS-EGCG-FA NPs)进行修饰。研究了 NPs 的粒径、形态、包封效率、流变性能、抗氧化和酪氨酸酶抑制活性。G-CS-EGCG-FA NPs 呈不规则椭圆形,平均直径为 412.3nm,具有较高的 DPPH 和 ABTS·清除能力。EGCG 和 FA 在 NPs 中的包封效率分别为 46.0±1.3%和 46.8±1.6%。CS 基 NPs 在浓度<200μg/mL 和 25μg/mL 时对 NIH 3T3 细胞和 B16-F10 黑色素瘤细胞无毒性作用,细胞活力在 100%至 118%之间。同时,G-CS-EGCG-FA NPs(200μg/mL)在 HO 诱导的细胞中的氧化修复能力超过 100%,高于相同剂量的游离 EGCG 或 FA。此外,G-CS-EGCG-FA NPs(25μg/mL)(84.6%)的酪氨酸酶抑制活性强于游离 EGCG(55.3%)、游离 FA(47.1%)和曲酸,表明 G-CS-EGCG-FA NPs 具有良好的皮肤修复和美白能力。鉴于这些结果,本研究为设计具有协同效益的双重生物活性物质载药新型粒子提供了新的思路。

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