Studies on the influence of penetration enhancers on in vitro permeation of carvedilol across rat abdominal skin

Order of Publishing in Issue: 
5
Volume :1
Issue :1
March, 2007
Page No: 
62-69
Authors: 
G. Ramesh, Vamshi Vishnu Y, Kishan V and Madhusudan Rao Y*
Address: 
Centre for Biopharmaceutics and Pharmacokinetics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal- 506 009 (A.P)
Email-ID: 
ymrao123@yahoo.com

The aim of the investigation was to study the effect of penetration enhancers on the in vitro permeation of carvedilol across excised ratabdominal skin and to select suitable penetration enhancer. Terpenes menthol, camphor, dlimoneneand carvone; surfactants, Transcutol and Labrasol at 5 % w/v, were used as penetration enhancers in the study. Skin permeation studieswere conducted in Franz diffusion cells using excised rat abdominal skin. Solutions containing 5 % w/v camphor showed maximum permeation(451.20 ?g?) in 24 hr with a flux of 5.23 ?g/hr/ cm2 and was significantly different (p<0.05) toflux obtained with other permeation enhancers. Control (phosphate buffer saline, pH 7.4containing 40 % v/v polyethylene glycol) sample showed lowest permeation (59.18 ?g?), with aflux of 0.67 ìg?/hr/cm2. The flux of carvedilol obtained from the solutions containing camphor,Transcutol, d-limonene, carvone, Labrasol and menthol (5 % w/v) were 7.81, 7.26, 6.52, 5.91,4.21 and 2.28 times higher than that observed with control, respectively. The flux obtained withcamphor was significantly higher (p<0.05) than the fluxes obtained with other penetrationenhancers. The present study suggests that camphor, Transcutol and d-limonene at 5 % w/vlevel may be used as penetration enhancers in the development of transdermal drug deliverysystems.

Keywords: 
Carvedilol, Terpenes, Transcutol, Labrasol, Rat skin.
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