Unraveling the Impact of the Oil Phase on the Physicochemical Stability and Skin Permeability of Melatonin Gel Formulations.

IF 5 3区 化学 Q1 POLYMER SCIENCE Gels Pub Date : 2024-09-16 DOI:10.3390/gels10090595
Juan J Torrado, Brayan J Anaya, Aytug Kara, Baris Ongoren, Sofía Esteban-Ruiz, Almudena Laguna, Alicia Guillén, Miguel G Saro, Dolores R Serrano
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Abstract

Melatonin's antioxidant properties make it a valuable component in anti-aging semisolid topical products. This study explores the role of Pemulen®, an acrylic-based viscosifying agent, in stabilizing cream-gel formulations. Remarkably, even at low concentrations (0.4%), Pemulen® successfully produced physicochemical stable topical formulations. In this work, the impact of the ratio of the oily phase-comprising olive oil and isopropyl myristate from 0 to 20%-was investigated to understand the internal microstructure effect on skin permeability, rheological properties, and stability. The formulations exhibited pseudoplastic behavior, with a significant positive correlation (p-value < 0.1) between the oily phase ratio, viscosity, spreadability, skin adhesiveness, and permeability. Formulations without the oil phase exhibited greater skin permeability. However, higher oily phase content enhanced viscosity, spreadability, and skin adhesion. Given that melatonin primarily degrades through oxidation, incorporating antioxidant excipients in semisolid formulations is crucial for maintaining its chemical stability. A quality by design (QbD) approach was used to assess the impact of four excipients-(a) DL-α-tocopheryl acetate (0.05%), (b) ascorbic acid (0.1%), (c) ethylene diamine tetraacetic acid (0.1%), and (d) sodium metabisulphite (0.5%)-on melatonin's stability. Our findings indicate that maintaining the physical stability of the formulation with a 20% oil phase is more critical for protecting melatonin from oxidation than merely adding antioxidant excipients.

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揭示油相对褪黑素凝胶配方理化稳定性和皮肤渗透性的影响
褪黑素的抗氧化特性使其成为抗衰老半固体外用产品的重要成分。本研究探讨了 Pemulen®(一种丙烯酸基增粘剂)在稳定膏霜凝胶配方中的作用。值得注意的是,即使浓度很低(0.4%),Pemulen® 也能成功地生产出理化性质稳定的外用配方。在这项研究中,为了了解内部微结构对皮肤渗透性、流变特性和稳定性的影响,研究了油性相(包括 0% 至 20% 的橄榄油和肉豆蔻酸异丙酯)比例的影响。配方表现出假塑性行为,油相比例、粘度、涂抹性、皮肤粘附性和渗透性之间存在显著的正相关性(p 值小于 0.1)。不含油相的配方具有更高的皮肤渗透性。然而,油相含量越高,粘度、涂抹性和皮肤粘附性就越强。鉴于褪黑素主要通过氧化降解,在半固体制剂中加入抗氧化辅料对保持其化学稳定性至关重要。我们采用质量源于设计(QbD)的方法评估了四种辅料--(a) DL-α-生育酚乙酸酯(0.05%)、(b) 抗坏血酸(0.1%)、(c) 乙二胺四乙酸(0.1%)和(d) 焦亚硫酸钠(0.5%)--对褪黑素稳定性的影响。我们的研究结果表明,在保护褪黑素不被氧化方面,保持配方中 20% 油相的物理稳定性比仅仅添加抗氧化辅料更为重要。
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来源期刊
Gels
Gels POLYMER SCIENCE-
CiteScore
4.70
自引率
19.60%
发文量
707
审稿时长
11 weeks
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