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http://dx.doi.org/10.4333/KPS.2003.33.1.029

The Effect of Enhancers on the Penetration of Clenbuterol through Hairless Mouse Skin  

Choi, Han-Gon (College of Pharmacy, Yeungnam University)
Rhee, Jong-Dal (College of Pharmacy, Yeungnam University)
Yu, Bong-Kyu (College of Pharmacy, Yeungnam University)
Yong, Chul-Soon (College of Pharmacy, Yeungnam University)
Publication Information
Journal of Pharmaceutical Investigation / v.33, no.1, 2003 , pp. 29-36 More about this Journal
Abstract
Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease, chronic bronchitis and pulmonary emphysema. The percutaneous permeation of clenbuterol was investigated in hairless mouse skin after application of 50/50 buffer(pH 10)/propylene glycol solvent mixture. The enhancing effects of various penetration enhancers such as terpenes, non-ionic surfactants, pyrrolidones, fatty acids and some other enhancers on the permeation of clenbuterol were evaluated using Franz diffusion cell. Among terpenes studied, 1,8-cineole was the most effective enhancer, which increased the permeability of clenbuterol approximately 39.33-fold compared with the control without penetration enhancer, followed by menthone with enhancement ratio of 23.57. Nonionic surfactants did not have significant enhancing effects. N-Lauryl-2-pyrrolidone increased the permeability of clenbuterol approximately 4.51-fold compared with the control. Lauric acid increased the permeability of clenbuterol approximately 35.57-fold with decreasing the lag time from 2.64 to 0.52 hr. Oleic acid, linoleic acid, linolenic acid and capric acid showed enhancement ratio of 22.62, 19.60, 17.45 and 16.51, respectively. $Labrafil^{\circledR}$ enhanced the permeability of clenbuterol 9.24-fold compared with that without enhancer.
Keywords
Clenbuterol; Enhancer; Transdermal drug delivery systems; Permeability;
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