Emulsification-based liposomal formulation of gallic acid and curcumin as potent topical antioxidants.

IF 1.5 Q3 PHARMACOLOGY & PHARMACY Drug Discoveries and Therapeutics Pub Date : 2025-03-06 Epub Date: 2025-02-26 DOI:10.5582/ddt.2025.01000
Takron Chantadee, Siripat Chaichit, Kanokwan Kiattisin, Worrapan Poomanee, Siriporn Okonogi, Pimpak Phumat
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Abstract

Excessive free radicals in the skin cause oxidative stress, damaging cells and leading to aging, melasma, and inflammation. This study developed a liposome system for co-delivering antioxidants to enhance their efficacy in deeper skin layers. Four phenolic compounds were screened for antioxidant activity using DPPH, nitric oxide scavenging, and lipid peroxidation assays. Gallic acid and curcumin, showing the strongest activity, were selected for liposome encapsulation via an emulsification method, with particle size reduction by probe sonication. High-performance liquid chromatography (HPLC) was used for chemical analysis, and particle morphology was examined with transmission electron microscopy. Studies on skin penetration, retention, and release were conducted. The optimized liposome (LP4) had a small particle size (< 150 nm), an unilamellar structure, and high entrapment efficiency (99% gallic acid and 92% curcumin). LP4 promoted effective skin retention of curcumin with slow penetration, while the release of gallic acid and curcumin from LP4 followed a Higuchi kinetic model and Zero-order kinetic model, respectively. This delivery system demonstrates potential for targeted antioxidant delivery, offering enhanced protection against oxidative damage in the skin.

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没食子酸和姜黄素作为有效的局部抗氧化剂的乳化型脂质体配方。
皮肤中过多的自由基会引起氧化应激,破坏细胞,导致衰老、黄褐斑和炎症。本研究开发了一种脂质体系统,用于共同输送抗氧化剂,以提高其在更深皮肤层的功效。通过DPPH、一氧化氮清除和脂质过氧化测定,筛选了四种酚类化合物的抗氧化活性。选择活性最强的没食子酸和姜黄素,通过乳化法包封脂质体,并通过探针超声缩小粒径。采用高效液相色谱法进行化学分析,透射电镜观察颗粒形态。对其皮肤渗透、滞留和释放进行了研究。优化后的脂质体(LP4)粒径小(< 150 nm),单层结构,包封效率高(没食子酸99%,姜黄素92%)。LP4促进姜黄素的有效皮肤滞留,但渗透缓慢,而没食子酸和姜黄素的释放分别符合Higuchi动力学模型和零级动力学模型。这种输送系统展示了靶向抗氧化输送的潜力,为皮肤的氧化损伤提供了增强的保护。
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来源期刊
Drug Discoveries and Therapeutics
Drug Discoveries and Therapeutics PHARMACOLOGY & PHARMACY-
CiteScore
3.20
自引率
3.20%
发文量
51
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