Yücel Çiğdem, Şeker Karatoprak Gökçe, Yalçıntaş Sena, Eren Böncü Tuğba
Faculty of Pharmacy, Department of Pharmaceutical Technology, Erciyes University, 38280 Kayseri, Turkey.
Faculty of Pharmacy, Department of Pharmacognosy, Erciyes University, 38280 Kayseri, Turkey.
Beilstein J Nanotechnol. 2022 May 31;13:491-502. doi: 10.3762/bjnano.13.41. eCollection 2022.
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.
含有天然化合物的控释系统已成功应用于化妆品中作为抗老化产品，以增强活性化合物透过皮肤的渗透能力。在本研究中，我们旨在开发含有一种强效抗氧化剂表没食子儿茶素-3-没食子酸酯（EGCG）的新型醇质体配方，并通过测定其抗氧化和抗老化作用来评估其在化妆品中的应用潜力。醇质体（ETHs）通过机械分散法制备，并在体外对其粒径（PS）、zeta电位（ZP）、多分散指数（PDI）、包封率百分比（EE%）和体外释放进行表征。最佳的ETH配方以1:1（v/v）的比例使用卡波姆980作为凝胶剂来制备醇质体基凝胶（ETHG）。对该凝胶配方的感官特性、pH值和粘度进行了评估。进行了为期三个月的稳定性研究，检查了ETHs的表征参数变化和残余EGCG含量。此外，对于ETHG，在三个月内测定其感官特性、pH值（每两周一次）和粘度（第一周和第十二周）。采用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）法测试配方和不同EGCG溶液对L929细胞系的细胞毒性。与溶液形式相比，研究了ETHs和ETHGs对胶原酶和弹性蛋白酶的细胞渗透特性及抑制作用。在抗氧化活性研究范围内，进行了2,2-二苯基-1-苦基肼（DPPH•）和2,2'-联氮-双-（3-乙基苯并噻唑啉-6-磺酸）（ABTS+•）自由基清除以及β-胡萝卜素/亚油酸共氧化抑制作用实验。优化后的负载EGCG的ETHs（F3）处于纳米尺度范围（238±1.10 nm）。最高包封率和体外释放值分别为51.7±1.15%和50.8±1.70%。ETHG成功地用编码为F3的ETHs配制而成，细胞毒性测试表明不同浓度的配方和EGCG溶液均无毒性。在细胞渗透性、酶抑制和抗氧化活性方面，醇质体配方比EGCG溶液产生了更好的结果。由于EGCG的稳定性，观察到配方具有长期效果。该研究结果强调了所开发的醇质体配方在化妆品领域的抗氧化和抗老化作用潜力。
