微乳改善硫辛酸和槲皮素在皮肤细胞和组织中的共定位和抗氧化作用

IF 3.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Mariana de Sousa Silva, Julia S. Passos, Regina G. Daré, Jessica R. Nunes, Patricia P. Adriani, Luciana B. Lopes
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引用次数: 0

摘要

槲皮素和α-硫辛酸是抗氧化剂,在治疗各种皮肤疾病,如伤口和皮肤癌的化学预防方面具有潜在的应用前景。为了使它们在组织中有效地局部共递送和共定位,我们开发了微乳液(ME)。所选择的ME (ME-50)形成了稳定的体系,平均液滴尺寸为134.4±17.9 nm,共加入抗氧化剂后,液滴尺寸增加到224.9±19.9 nm。ME保留了分子的抗氧化能力,清除DPPH(2,2-二苯基-1-picrylhydrazyl)的IC50为6.2±0.1µg/mL,与溶液相似。皮肤渗透研究显示,与对照溶液相比,经过12小时的ME处理后,角质层中槲皮素(Q)的积累增加了2.4倍,向活表皮和真皮(ED)的递送增加了3.5倍;α-硫辛酸(LA)在ED中的渗透率提高了1.9倍。Q + LA共载ME处理角质层和ED的抗氧化活性分别比溶液提高1.3倍和2.0倍。与对照(未处理)细胞相比,在暴露于h2o2的角质形成细胞中,ME处理24小时也使氧化物种水平降低了55%。综上所述,这些结果表明ME-50是一种很有前途的递送系统,可以增强槲皮素和α-硫辛酸的皮肤共递送和组织中的抗氧化作用,为氧化应激相关皮肤疾病提供潜在的局部治疗。图形抽象
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Microemulsions Improve the Cutaneous Co-Localization of Lipoic Acid and Quercetin and Antioxidant Effects in Cutaneous Cells and Tissue

Microemulsions Improve the Cutaneous Co-Localization of Lipoic Acid and Quercetin and Antioxidant Effects in Cutaneous Cells and Tissue

Quercetin and α-lipoic acid are antioxidants with potential applications in the treatment of various skin conditions, such as wounds and chemoprevention of skin cancer. To enable their effective topical co-delivery and co-localization in the tissue, we developed microemulsions (ME). The selected ME (ME-50) formed a stable system with a mean droplet size of 134.4 ± 17.9 nm, increasing to 224.9 ± 19.9 nm upon antioxidants co-incorporation. The ME preserved the antioxidant capacities of the molecules, with DPPH (2,2-diphenyl-1-picrylhydrazyl) scavenging assay showing an IC50 of 6.2 ± 0.1 µg/mL, similar to the solution. Skin penetration studies revealed a 2.4-fold increase in quercetin (Q) accumulation in the stratum corneum and a 3.5-fold increase in the delivery to viable epidermis and dermis (ED) after a 12 h-treatment with the ME compared to control solutions; α-lipoic acid (LA) penetration improved up to 1.9-fold in ED upon ME incorporation. Treatment with Q + LA co-loaded ME enhanced the antioxidant activity in the stratum corneum and ED by 1.3-fold and 2.0-fold, respectively, compared to solutions. Treatment with the ME for 24 h also reduced oxidative species levels by 55% in H2O2-exposed keratinocytes compared to the control (untreated) cells. Taken together, these results suggest that ME-50 is a promising delivery system for enhancing the cutaneous co-delivery of quercetin and α-lipoic acid and the antioxidant effects in the tissue, offering a potential topical treatment for oxidative stress-related skin conditions.

Graphical Abstract

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来源期刊
AAPS PharmSciTech
AAPS PharmSciTech 医学-药学
CiteScore
6.80
自引率
3.00%
发文量
264
审稿时长
2.4 months
期刊介绍: AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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