Ethosomal (−)-epigallocatechin-3-gallate as a novel approach to enhance antioxidant, anti-collagenase and anti-elastase effects

Abstract

Controlled release systems containing natural compounds have been successfully applied in cosmetics as antiaging products to enhance the penetration of active compounds through the skin. In this study, we aimed to develop novel ethosomal formulations containing a potent antioxidant, epigallocatechin-3-gallate (EGCG), and to evaluate their potential for use in cosmetics by determining their antioxidant and antiaging effects. Ethosomes (ETHs) were prepared via mechanical dispersion and characterized in vitro in terms of particle size (PS), zeta potential (ZP), polydispersity index (PDI), encapsulation efficiency percentage (EE%), and in vitro release. The best ETH formulation was used to prepare the ethosome-based gel (ETHG) by using Carbopol 980 as a gelling agent at a ratio of 1:1 (v/v). The gel formulation was evaluated regarding organoleptic properties, pH values, and viscosity. Stability studies were conducted for three months and changes in characterization parameters and residual EGCG content of ETHs were examined. Besides, for ETHG, organoleptic properties, pH values (every two weeks), and viscosity (first and twelfth week) were determined for three months. The 3-(4,5-dimethyldiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to test the cytotoxicity of the formulations and different EGCG solutions on the L929 cell line. The cell permeation properties and inhibitory effects of ETHs and ETHGs on collagenase and elastase enzymes were investigated compared to those of the solution form. Within the scope of antioxidant activity studies, 2,2-diphenyl-1-picrylhydrazyl (DPPH•) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+•) radical scavenging and β-carotene/linoleic acid co-oxidation inhibitory effects were carried out. The optimized EGCG-loaded ETHs (F3) were within the nanoscale range (238 ± 1.10 nm). The highest encapsulation efficiency and in vitro release values were 51.7 ± 1.15% and 50.8 ± 1.70%, respectively. The ETHG was successfully formulated with F3-coded ETHs and the cytotoxicity test revealed that the formulations and the EGCG solution at different concentrations were nontoxic. In terms of cell permeability, enzyme inhibition, and antioxidant activity, the ethosomal formulations yielded better results compared to the EGCG solution. It was observed that the formulations had a long-term effect due to the stability of EGCG. The findings of the study underline the potential of antioxidant and antiaging effects of the developed ethosomal formulations for use in the cosmetic field.

Antioxidant Effects of Catechins (EGCG), Andrographolide, and Curcuminoids Compounds for Skin Protection, Cosmetics, and Dermatological Uses: An Update

“…[73] Use of ethosomes To protect EGCG from environmental aggressions. [74,75] Similar study on niosome-loaded EGCG To improve skin penetration and protect encapsulated molecules. [22] Table 4.…”

“…The limited availability of these agents can be overcome by working on cosmetic formulations of the emulsion [73], encapsulation, and micro or nanoparticles type, which allow excellent penetration of all skin layers. To improve penetration, EGCG was formulated by Boncu et al [74] in controlled-release systems for anti-aging cosmetic applications using ethosome-based formulations. These were prepared by mechanical dispersion with a gelling agent, Carbopol 980.…”

Elastase and COVID-19 relationship, and potential natural resource as elastase inhibitors: A comprehensive review

“…So far, several secondary metabolites that have been identified have potential elastase inhibitor activity, such as polyphenols, flavonoids, tannins, and triterpenoids [84,87,88,92,93,[95][96][97]99,110,[112][113][114][115][116][117][118]. Some active compounds as elastase inhibitors from these compound groups have been isolated and identified, such as agrimoniin, pedunculagin, epigallocatechin gallate, resveratrol, genistein, parthenolide from Tormetillae Rhizoma [119]; Pyracrenic acid, catechin, piceatannol, arjunolic acid, and betulinic acid from the stems of Callistemon lanceolatus [89]; Maslinic acid, betulinic acid, and 2-hydroxynaringenin-7-O-β-D-glucopyranoside from Cornus kousa [120]; Visconata from Dodonaea viscosa [97]; Hydroxyhibiscone A from Hibiscus syriacus [99]; and ellagitannin from Melaleuca styphelioides [96].…”

Strategies to Enhance Drug Pass in Transdermal and Dermal Therapeutic Systems: Traditional Review

“…Yapılarındaki etanol dermal ve transdermal sistemlerde ilaçların daha derin katmanlara geçmesine sebep olabilir. 34 Etanol, SK lipid moleküllerinin sıkı düzenini değiştirebilir ve lipid akışkanlığını artırır. 18…”