Hesperetin微乳劑及霜劑配方對於經皮吸收及美白評估

Investigation of microemulsion and cream formulations as carriers of hesperetin in permeation and whitening evaluation

李科鋒(Ko-Feng Lee)

指導教授 ： 吳寶珠

高雄醫學大學/藥學院/藥學研究所/碩士(2008年)

摘要

Hesperetin大多存在於柑橘類中，是目前最常被研究的天然物質，許多研究指出hesperetin具有抑制xanthine oxidase及tryosinase等酵素之作用，對於抗老化和美白等改善皮膚機能上確實具有潛力。將hesperetin製成霜劑及微乳劑，利用體外穿透實驗評估藥物經鼠皮的穿透率（flux）、累積穿透量（Q）、延滯時間（lag time）、皮內含量等參數，篩選較佳的霜劑及微乳劑處方，進行配方美白、刺激性及配方安定性等實驗。在體外穿透實驗評估中，霜劑處方C1（含有2.5% menthol、2.5% linoleic acid及2.5% lecithin）及微乳劑處方F10（含有3% padimate O），兩者具有較高的flux及較小的lag time，故選用此兩者處方進行配方美白、刺激性及配方安定性等實驗。在美白實驗：抑制酪胺酸酶及還原已生成黑色素能力中發現，投予霜劑處方C1及微乳劑處方F10後，能使皮膚亮度提升。在皮膚刺激性方面，C1及F10會降低水份散失速率，且處方不會引起發紅反應，顯示C1及F10在此動物模式中不具刺激性。在安定性實驗方面，微乳劑處方F10在放置兩個月後其粒徑大小仍維持不變大約為128 nm而且藥物含量維持在97.97%。霜劑處方C1在放置兩個月後處方外觀顏色不變及藥物含量維持在98.84%，證明兩者處方皆為安定。

關鍵字

Hesperetin ； 霜劑 ； 微乳劑 ； 經皮吸收

並列摘要

Recently, people attach importance to anti-aging and whitening effect not only in beauty but also in healthy. More and more evidence to point out antioxidant and antityrosinase activities can postpone aging and make whitening. Hesperetin, a flavanone compound, is almost exclusively present in citrus fruits and it has good antityrosinase and antioxidant activities. In this study, hesperetin of creams and microemulsions were prepared and evaluated the permeation parameters through rat skin in vitro study, skin whitening, skin irritation and stability of experimental formulations. In vitro permeation studies, the cream (C1, containing 2.5% menthol, 2.5% linoleic acid and 2.5% lecithin) and microemulsion (F10, containing 3% padimate O) formulations have higher flux and short lag time, so we choose these formulations to proceed with whitening, skin irritation and stability study. In whitening study including tyrosinase inhibition activity and reduce pigmentation study, the ∆L＊(∆L＊= L＊of reading - Pre-exposure L＊) were increased after topical application of C1 and F10 formulations, indicated C1 and F10 had whitening effect. In skin irritation study, C1 and F10 could decrease transdermal water loss after UV exposure and did not induce inflamed effect. These results indicated our formulations have no skin irritation in these animal models. The result of stability study in two months storage showed that average particle size of F10 maintained at 128 nm, and content of hesperetin maintained at 97.97%. The outward appearance of C1 did not change after two months storage and content of hesperetin maintained at 98.84%.

並列關鍵字

Hesperetin ； Cream ； Microemulsion ； transdermal

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