Effect of permeation enhancers and organic acids on the skin permeation of indapamide.
The aim of present study was to investigate the transdermal properties of indapamide and to explore the efficacy of various permeation enhancers and organic acids with regard to the percutaneous absorption of indapamide. Permeation experiments were performed in vitro, using rat abdominal skin as a barrier. In the permeation studies, 2-chamber diffusion cells were used. The results obtained indicate that N-dodecylazepan-2-one, N-methyl-2-pyrrolidone, menthol and oleic acid had a strong enhancing effect on the permeation of indapamide and N-dodecylazepan-2-one exhibited the most potent enhancing effect. All eight of the organic acids chosen had a potent enhancing effect on the permeation of indapamide across rat abdominal skin. Among the organic acids examined, lactic acid had the greatest enhancing effect. The formation of an ion-pair between indapamide and organic acids may be responsible for the enhanced skin permeation of indapamide. Although the exact reason remains unknown, it is worth carrying out further investigations.
Ren
Changshun
C
Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, China.
Fang
Liang
L
Li
Ting
T
Wang
Manli
M
Zhao
Ligang
L
He
Zhonggui
Z
D000143:Acids / Q000494:pharmacology; D000818:Animals; D000431:Ethanol / Q000494:pharmacology; D007190:Indapamide / Q000493:pharmacokinetics*; D008297:Male; D009930:Organic Chemicals / Q000494:pharmacology; D010539:Permeability; D019946:Propylene Glycol / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption; D012995:Solubility
D000143:Acids; D009930:Organic Chemicals; D000431:Ethanol; D019946:Propylene Glycol; D007190:Indapamide