Development of Transethosomes Delivery System Loaded with Bouea macrophylla Griffith Seed Kernel Extract for Cosmeceutical Application

Phattharawadee Jaikham, P. Leelapornpisid, Worrapan Poomanee
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Abstract

This research aimed to develop and optimize transethosomes loaded with Bouea macrophylla Griffith seed kernel extract (B-SE). Firstly, extraction procedures using solvent fractionation with various polarity: hexane, ethyl acetate and 95% (v/v) ethanol. The physicochemical properties of B-SE were investigated in terms of partition coefficient (LogP), solubility and pH-stability. To optimize the transethosomes formulation, the compositions were varied in sorts of percent cosurfactant, types of cosurfactant, extract concentration, percent total surfactant and types of particle ingredients (phospholipid or cholesterol). The significant factors influencing physical characteristics of the transethosomes were statistically identified using the 25-1 fractional factorial design. Particle size, polydispersity index (PDI), percent entrapment efficiency (%EE) and ultrastructural morphology of the optimized formulation was then characterized. As a marker of B-SE, ellagic acid (EA) was identified by HPLC at a retention time of 32.506 ± 0.16 min. The LogP of B-SE was 0.17. B-SE was practically insoluble in water but freely soluble in propylene glycol and ethanol. The pH condition that stabilized the extract was pH-5. The optimized formulation, consisted of phospholipid, propylene glycol, TWEEN 20, SPAN 80 and 2.5 mg/ml of B-SE presenting particle sizes of 79.72 ± 2.42 nm, PDI of 0.26±0.02 and %EE of 83.10±0.03% along with a spherical particle shape. To conclude, the optimized transethosomes loaded with B-SE fabricated by phospholipid and propylene glycol has desirable attributes for further developing into an anti-acne cosmeceutical. Nonetheless, the bioactivities and safety profile of the transethosomes were necessary for further investigation. Keywords: Bouea macrophylla Griffith, Transethosomes, Ellagic acid, Fractional factorial design, Nanocarrier
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开发用于化妆品应用的含有大叶黄杨格里菲斯籽仁提取物的 Transethosomes 递送系统
本研究旨在开发和优化含有大叶女贞子种仁提取物(Bouea macrophylla Griffith seed kernel extract,B-SE)的透硫体。首先,采用正己烷、乙酸乙酯和 95% (v/v) 乙醇等不同极性的溶剂分馏提取程序。研究了 B-SE 的分配系数(LogP)、溶解度和 pH 稳定性等理化特性。为了优化反式硫体的配方,改变了共表面活性剂的百分比、共表面活性剂的类型、提取物的浓度、表面活性剂的总百分比和颗粒成分的类型(磷脂或胆固醇)。采用 25-1 分因子设计对影响反式硫体物理特性的重要因素进行了统计。然后对优化配方的粒度、多分散指数(PDI)、夹带效率百分比(%EE)和超微结构形态进行了表征。作为 B-SE 的标记物,鞣花酸(EA)经 HPLC 鉴定,保留时间为 32.506 ± 0.16 分钟。B-SE 的 LogP 为 0.17。B-SE 几乎不溶于水,但可自由溶于丙二醇和乙醇。使提取物稳定的 pH 值为 pH-5。优化配方由磷脂、丙二醇、TWEEN 20、SPAN 80 和 2.5 mg/ml 的 B-SE 组成,粒径为 79.72 ± 2.42 nm,PDI 为 0.26±0.02,%EE 为 83.10±0.03%,呈球形颗粒。总之,用磷脂和丙二醇制造的负载 B-SE 的优化反式硫体具有理想的属性,可进一步开发成抗痤疮药用化妆品。尽管如此,仍有必要进一步研究反式硫化小体的生物活性和安全性。关键词格里菲斯大叶榕 反式硫体 鞣花酸 分因子设计 纳米载体
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