環糊精7‚8‚4′-Trihydroxyisoflavone包合物的安定性及其抗氧化活性之探討

Investigation of the stability and antioxidant activity in various cyclodextrins with 7‚8‚4′-Trihydroxyisoflavone inclusion complex

許芷瑀(Chih-Yu Hsu)

指導教授 ： 顏峰霖

高雄醫學大學/藥學院/香粧品學系碩士班/碩士(2017年)

摘要

7,8,4′-Trihydroxyisoflavone (784THIF)為異黃酮中daidzein的二次代謝產物。先前研究發現784THIF有許多生物活性，包含抗氧化及抗發炎等功效。然而，784THIF有許多缺點如:難溶於水、穩定性差、生物利用性低，因此限制了它在醫藥、食品、化粧品工業上的運用。本研究主要以不同環糊精，包含α-cyclodextrin、β-cyclodextrin、γ-cyclodextrin、hydroxypropyl-β-cyclodextrin (HPBCD)作為載體來包合784THIF，並探討其溶解度、穩定性、皮膚吸收以及抗氧化活性的關係。本實驗結果顯示Hydroxypropyl-β-cyclodextrin (HPBCD)784THIF包合物(HP-784)的包合能力及溶解度優於其他環糊精是藉由改善物理化學性質如，784THIF與HPBCD之分子間氫鍵鍵結、無晶型形成。此外， HP-784的經皮吸收優於β環糊精784THIF 包合物(B-784)與784THIF粉末而HP-784在光安定性及溫度穩定性也呈現出較佳的表現且有效地維持其抗氧化之活性。結論，HP-784包合物可做為化粧品添加劑並用來保養皮膚。

關鍵字

7,8,4′-Trihydroxyisoflavone ； 環糊精 ； 包合物 ； 溶解度 ； 安定性 ； 抗氧化活性

並列摘要

7,8,4'-Trihydroxyisoflavone (784THIF), a secondary metabolite from daidzin, has been found many biological activities, including antioxidant and anti-inflammation. However, 784THIF has aqueous poor solubility, stability and bad bioavailability to limit its application in medicine, food and cosmetic industry. The purpose of the study is used various cyclodextrins, including α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin, hydroxypropyl-β-cyclodextrin (HPBCD), as a carrier to inclusion 784THIF and investigated the improvement of aqueous solubility, stability, skin absorption and antioxidant activity. The results of the present study indicated that hydroxypropyl-β-cyclodextrin 784THIF inclusion complex (HP-784) presents the best inclusion efficiency and aqueous solubility than other cyclodextrins by improving the physicochemical properties, such as amorphous transformation, hydrogen bonding interaction with HPBCD. In addition, HP-784 also increased the in vitro skin penetration when compared with raw 784THIF and β-cyclodextrin inclusion complex (B-784). HP-784 had better photostability and thermalstability than raw 784THIF in alcohol and which can maintain the antioxidant activity of 784THIF. In conclusion, HP-784 inclusion complex may be used as an additive in cosmetic product to care skin.

並列關鍵字

7,8,4′-Trihydroxyisoflavone ； cyclodextrins ； inclusion complex ； solubility ； stability ； antioxidant

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