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  • 學位論文

搭載白藜蘆醇與阿魏酸的奈米脂質載體的製備及功效

Preparation and functions of resveratrol-ferulic acid loaded nanostructured lipid carrier system

指導教授 : 蔣丙煌
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摘要


近年來消費者對以天然成分為訴求的皮膚保養品的需求愈來愈高,尤其是具有美白效果的天然保養品在亞洲市場的需求量甚大。在亞洲人眼中,皮膚白皙代表的不僅是美,還隱含了社會階層的標誌。天然的植化素中,阿魏酸與白藜蘆醇已被多個研究證實能有效地抑制紫外線照射引起的物質變性、清除自由基、抑制氧化反應和自由基反應、抑制酪氨酸酶的活動,從而抑制黑色素的生成。保養品多直接使用於皮膚,但皮膚不易穿透的特性卻讓保養品中的有效成分的吸收受到限制。因此,如何使有效的活性物質順利穿透表層皮膚組織到達作用位置極其重要。本研究結合多重乳化技術與奈米結構脂質載體的概念,利用超音波探針均質,製造出同時搭載親脂性與親水性植化素的奈米脂質載體 (nanostructured lipid carrier)。 本研究選用的天然來源原料包括以利普脂、癸酸三酸甘油酯、親脂性乳化劑聚甘油-4異硬脂酸酯(polyglyceryl-4 isostearate) 及親水性乳化劑聚甘油-3甲基葡萄糖二硬脂酸酯(polyglyceryl-3 methylglucose distearate)。在全因子實驗設計的優化下,當聚甘油-3甲基葡萄糖二硬脂酸酯的濃度為2.56%與第二階段超音波均質時間為6分鐘時,奈米脂質載體之粒徑為375.37 ± 90.26 nm,穩定度為94.29% ± 1.39, 阿魏酸包埋率為85.49% ± 8.45,白藜蘆醇包埋率為85.57% ± 1.39。將上述優化的載體配方進行經皮吸收試驗(豬背皮),載體組與控制組相比,白藜蘆醇的穿透量增加了29.31%。而利用膠帶撕貼法的人體經皮吸收試驗,證實了載體組中阿魏酸及白藜蘆醇的穿透率比控制組分別高出17.23%及27.19%。後續的細胞實驗也證實了阿魏酸及白藜蘆醇確實對UVA照射誘導小鼠B16F10黑色素瘤細胞生成黑色素有抑制的作用。本研究的結果提供了以天然來源原料製備搭載植化素的的奈米脂質載體的方法,以及提升了其用於美白保養品的可行性。

並列摘要


Surging consumer demand for skin care product that are free from harmful chemicals has encouraged the development of product derived from natural sources. Among all the product benefits skin lightening has gained a lot of attention in the last years, especially in Asian communities. Topically applied product, however, often suffer from low penetration of active compounds into skin due to excellent barrier of stratum corneum. In an attempt to overcome these problems, this study has developed a nanostructured lipid carriers (NLC) system encapsulating both hydrophilic ferulic acid and lipophilic resveratrol. Both of these two compounds are known to be able to inhibit melanogensis in skin. Natural derived ingredients including illipe nut butter, capric triglyceride, polyglyceryl 4 isostearate, and polyglyceryl 3 methylglucose distearate were chosen to fabricate NLC. A full factorial design was used to optimize the concentration of polyglyceryl 3 methylglucose distearate and duration of ultrasonication during second stage of emulsification. Results showed that 2.56% of polyglyceryl 3 methylglucose distearate and 6 minutes sonication time were suitable to produce stable NLC system with mean diameter of 375.37 ± 90.26 nm, 94.29% ± 1.39 stability, 85.49% ± 8.45 ferulic acid encapsulation efficiency, and 85.57% ± 1.39 resveratrol encapsulation efficiency. The ex vivo penetration study revealed that NLC could increase the penetration of resveratrol for about 29.31% in porcine back skin. The in vivo tape stripping penetration study indicated that the NLC increased the cumulative penetration of ferulic acid and resveratrol by 17.23% and 27.19% respectively as compared to the free compounds. The in vitro antimelanogenic effects of ferulic acid and resveratrol was demonstrated by treating B16F10 mouse melanoma cells with different amount of these phytochemicals loaded NLC before and after exposure to UVA radiations. These findings suggested that NLC made by natural derived ingredients is a promising topical delivery system that had a potent enhancement effect for ferulic acid-resveratrol penetration into skin.

參考文獻


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