Grape Seed Oil Microemulsion for Improved Skin Delivery of Resveratrol.

IF 4 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Marianne A P C Nogueira, Camila O Cardoso, Lucas F F Albuquerque, Marcilio Cunha-Filho, Tais Gratieri, Guilherme M Gelfuso
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Abstract

Given the anti-inflammatory properties of Resveratrol, this paper proposes developing a grape seed oil-in-water microemulsion (ME) for topical administration to treat inflammatory skin pathological conditions. Thermal analyses confirmed compatibility between Resveratrol, grape seed oil, Tween 80, and Span 80 used in the formulations. Two compositions (ME1 and ME2) were selected from a pseudo-ternary diagram prepared by components titration. ME1 (50% water, 35% surfactant, 15% oil) and ME2 (60% water, 30% surfactant, 10% oil) showed mean droplet sizes of 23.1 ± 0.7 nm and 24.9 ± 1.7 nm (PdI = 0.34 and 0.47), zeta potential between -11.7 ± 0.5 and -13.6 ± 0.9 mV, and pH values of 6.2 ± 0.5 and 7.1 ± 1.1, respectively. Rheological analyses revealed Newtonian behavior and low viscosity, with physical stability for 60 days at room temperature. In vitro drug permeation studies using porcine skin demonstrated that ME increased Resveratrol penetration into deeper skin layers by fourfold (p < 0.001) compared to the control solution (ME1: 2.9 ± 0.1 μg/cm2, ME2: 2.4 ± 0.1 μg/cm2), while reducing retention in the stratum corneum. HET-CAM experiments indicated safety for topical application. In conclusion, the ME was a promising alternative for future clinical investigations to treat inflammatory skin conditions.

葡萄籽油微乳液用于改善白藜芦醇的皮肤输送。
鉴于白藜芦醇的抗炎作用,本文建议研制一种葡萄籽水包油微乳(ME),用于外用治疗皮肤炎性病变。热分析证实了白藜芦醇、葡萄籽油、Tween 80和Span 80在配方中的相容性。用组分滴定法从拟三元图中筛选出ME1和ME2两种组分。ME1(50%水、35%表面活性剂、15%油)和ME2(60%水、30%表面活性剂、10%油)的平均液滴尺寸分别为23.1±0.7 nm和24.9±1.7 nm (PdI分别为0.34和0.47),zeta电位在-11.7±0.5和-13.6±0.9 mV之间,pH值分别为6.2±0.5和7.1±1.1。流变学分析显示其具有牛顿特性和低粘度,在室温下具有60天的物理稳定性。猪皮肤的体外药物渗透研究表明,ME2使白藜芦醇在皮肤深层的渗透增加了4倍(p 2, ME2: 2.4±0.1 μg/cm2),同时减少了在角质层的滞留。HET-CAM实验表明外用安全。总之,在未来的临床研究中,ME是一种治疗炎症性皮肤疾病的有希望的替代方法。
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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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