경피용 프로드럭인 에칠 글리콜레이트의 국소자극 및 피부투과성

• 영문명: Skin Penetration and Local Irritation of Ethyl Glycolate, a Potential Transdermal Prodrug
• 발행기관: 대한약학회
• 저자명: 양성운(Sung Woon Yang) 하용호(Yong Ho Ha) 김종갑(Johng Kap Kim) 최영욱(Young Wook Choi)
• 간행물 정보: 『약학회지』제40권 제2호 (1996년), 155~162쪽, 전체 8쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1996.04.30

영문 초록

Hyperkeratinization is a dermatologic disorder, which is due to the increase of corneocyte cohesion force. Glycolic acid, an alpha hydroxy acid(AHA), has been used to breakdown the hyperkeratinization processes. However, it has a problem of skin irritation when applied topically, due to the strong acidity especially in high concentration. A molecular optimization of glycolic acid has been tried to reduce the skin irritation by the way of prodrug formation. Ethyl glycolate was synthesized by the esterification of glycolic acid with ethanol in acidic conditions in the presence of sulfuric acid, and examined under the spectroscopic trials, such as UV, IR, 1H-NMR, and GC-MS. The physicochemical and biopharmaceutical properties of the prodrug were also evaluated. Through the toxicological tests of both skin irritation and eye mucous irritation, it has been proved that ethyl glycolate was less irritant than glycolic acid, since the pH value of synthetic prodrug was higher than that of glycolic acid. In the penetration test through nude mouse skin by diffusion cell, ethyl glycolate was continuously hydrolyzed to glycolic acid, which was assayed form the receptor compartment. It was obtained that the penetrated amount of ethyl glycolate was five times higher than that of glycolic acid. These results suggest that ethyl glycolate might be a successful prodrug of glycolic acid to reduce the skin irritation and to increase the skin penetration as well.

키워드

Glycolic acid Ethyl glycolate Hyperkeratinization Skin penetration Local irritation Prodrug.