白藜蘆醇微乳劑的經皮輸送評估

Study of Resveratrol-loaded microemulsions for transdermal drug delivery

盧奕儒(Yi-Ru Lu)

指導教授 ： 吳寶珠

高雄醫學大學/藥學院/藥學系碩士班/碩士(2015年)

摘要

Resveratrol(白藜蘆醇)是一個多酚類的化合物，通常存在於葡萄、花生和紅酒等食物當中。過去研究指出，Resveratrol具有心血管保護作用、抗發炎和抗癌等作用，除此之外亦能夠移除自由基、阻止自由基的生成，因此在抗老化、抗氧化的研究中相當受到矚目。但是由於Resveratrol對水的溶解度低以及口服生體可用率低等缺點，而造成它在使用上有許多的限制和阻礙，本研究擬藉由微乳劑作為藥物載體，以經皮輸送系統來改善目前的缺點。微乳劑作為藥物輸送載體有許多優點，如增加藥物溶解度、提升皮膚滲透度，進而改善生體可用率和容易製造等。研究中會進行處方物化性質評估，安定性、刺激性評估及體外穿皮試驗評估，以了解微乳劑劑型對藥物的經皮累積穿透量及皮膚沈積量之影響，並評估其可用性。由結果顯示，處方F5和F6，具有不錯的經皮累積穿透量及皮膚沈積量，在皮膚刺激性的部分顯示處方對皮膚並不會造成太大的破壞或損傷，而在安定性結果顯示，兩者皆具有一定的穩定性，因此我們能藉由經皮輸送系統來提升Resveratrol的生體可用率，並且使它能有更多的應用。

關鍵字

白藜蘆醇 ； 微乳劑 ； 經皮吸收

並列摘要

Resveratrol is a polyphenol compound found in various common foods like grapes, peanuts and red wine. It had cardio-protective, anti- inflammatory and anticancer activities. But resveratrol was poorly soluble in water and low bioavailability which limited its oral utility. In this study, microemulsion was used as carrier to transport resveratrol through skin. Microemulsion provided several advantages for transdermal drug delivery, such as increased drug solubility, enhanced skin penetration, improved the bioavailability and easy to prepare. The physicochemical properties, in vitro skin permeation, stability and caused skin irritation of drug-loading microemulsions were determined to evaluate its utility. The result showed that formulation F5 and F6 had higher skin permeation amount and higher disposition amount in skin. Both formulations also showed stable after three stability tests and didn’t cause significant ittiratation after 24hr application. Therefore, we can use transdermal delivery system to enhance drug bioavailability.

並列關鍵字

Resveratrol ； Microemulsion ； Transdermal drug delivery

參考文獻

1. Park EJ, Pezzuto JM. The pharmacology of resveratrol in animals and humans. Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease. 2015;1852(6):1071-113.

2. Barrajón-Catalán E, Menéndez-Gutiérrez MP, Falco A, Carrato A, Saceda M, Micol V. Selective death of human breast cancer cells by lytic immunoliposomes: Correlation with their HER2 expression level. Cancer Letters. 2010;290(2):192-203.

3. Aïssaoui R, Fabian F. The French Paradox: Implications for Variations in Global Convergence. Journal of International Management. 2015;21(1):31-48.

4. Belleville J. The French paradox: possible involvement of ethanol in the protective effect against cardiovascular diseases. Nutrition. 2002;18(2):173-7.

5. Summerlin N, Soo E, Thakur S, Qu Z, Jambhrunkar S, Popat A. Resveratrol nanoformulations: Challenges and opportunities. International Journal of Pharmaceutics. 2015;479(2):282-90.