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用于增强表没食子儿茶素没食子酸酯经皮递送以抵御皮肤氧化应激的脂质体纳米载体

Niosomal Nanocarriers for Enhanced Dermal Delivery of Epigallocatechin Gallate for Protection against Oxidative Stress of the Skin.

作者信息

Li Danhui, Martini Nataly, Wu Zimei, Chen Shuo, Falconer James Robert, Locke Michelle, Zhang Zhiwen, Wen Jingyuan

机构信息

School of Pharmacy, Faculty of Medical and Health Sciences, The University of Auckland, Auckland 1023, New Zealand.

Department of Plastic, School of Pharmacy, The University of Queensland, Pharmacy Australia Centre of Excellence, Brisbane, QLD 4102, Australia.

出版信息

Pharmaceutics. 2022 Mar 28;14(4):726. doi: 10.3390/pharmaceutics14040726.

Abstract

Among green tea catechins, epigallocatechin gallate (EGCG) is the most abundant and has the highest biological activities. This study aims to develop and statistically optimise an EGCG-loaded niosomal system to overcome the cutaneous barriers and provide an antioxidant effect. EGCG-niosomes were prepared by thin film hydration method and statistically optimised. The niosomes were characterised for size, zeta potential, morphology and entrapment efficiency. Ex vivo permeation and deposition studies were conducted using full-thickness human skin. Cell viability, lipid peroxidation, antioxidant enzyme activities after UVA-irradiation and cellular uptake were determined. The optimised niosomes were spherical and had a relatively uniform size of 235.4 ± 15.64 nm, with a zeta potential of -45.2 ± 0.03 mV and an EE of 53.05 ± 4.46%. The niosomes effectively prolonged drug release and demonstrated much greater skin penetration and deposition than free EGCG. They also increased cell survival after UVA-irradiation, reduced lipid peroxidation, and increased the antioxidant enzymes' activities in human dermal fibroblasts (Fbs) compared to free EGCG. Finally, the uptake of niosomes was via energy-dependent endocytosis. The optimised niosomes have the potential to be used as a dermal carrier for antioxidants and other therapeutic compounds in the pharmaceutical and cosmetic industries.

摘要

在绿茶儿茶素中,表没食子儿茶素没食子酸酯(EGCG)含量最为丰富,且具有最高的生物活性。本研究旨在开发并通过统计学方法优化负载EGCG的非离子表面活性剂囊泡系统,以克服皮肤屏障并发挥抗氧化作用。采用薄膜水化法制备EGCG非离子表面活性剂囊泡并进行统计学优化。对囊泡的大小、zeta电位、形态和包封率进行表征。使用全层人皮进行体外渗透和沉积研究。测定细胞活力、脂质过氧化、紫外线A照射后的抗氧化酶活性以及细胞摄取情况。优化后的囊泡呈球形,大小相对均匀,为235.4±15.64nm,zeta电位为-45.2±0.03mV,包封率为53.05±4.46%。与游离EGCG相比,囊泡有效地延长了药物释放,并表现出更强的皮肤渗透和沉积能力。它们还提高了紫外线A照射后的细胞存活率,减少了脂质过氧化,并增加了人皮肤成纤维细胞(Fbs)中抗氧化酶的活性。最后,囊泡的摄取是通过能量依赖的内吞作用进行的。优化后的囊泡有潜力在制药和化妆品行业用作抗氧化剂及其他治疗性化合物的皮肤载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71c3/9029719/eafdc0bb0bc9/pharmaceutics-14-00726-g001.jpg

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