Abstract
THE EFFECT OF CHEMICAL PENETRATION ENHANCERS ON THE PERCUTANEOUS ABSORPTION OF CARVEDILOL

Eskandar Moghimipour, Marzieh Mahmoodi and Anayatollah Salimi*

ABSTRACT

Carvedilol is a cardio-selective beta-blocker that is used to treat high blood pressure and heart failure. It has a protein binding of more than 98%. Its bioavailability is less than 23% during oral use, with a duration of action of about 6 hours. Transdermal drug delivery has advantages over oral dosing, which includes no first-pass liver metabolism and continuous drug release. In this study, the effect of chemical penetration enhancers on the permeability and skin absorption of carvedilol is investigated. Labrazol, labrafil, labrafac, Castor oil, and oleic acid were used as chemical penetration enhancers and rat skin was used as an animal model. The effect of enhancers on skin structure was studied by using DSC technique. The results of the permeability parameters showed that the highest permeation amount obtained from labrafac. The amount of flux and partitioning compared to control increased, as well as all chemical enhancers decreases the lag time compared to control. Castor oil had the least effect on increasing the drug's permeability from the skin. The result of the DSC technique also confirmed the same results. The use of chemical enhancers due to changes the structure of the skin to increase the permeability of the drug can be considered as suitable excipients in transdermal delivery of carvedilol.

Keywords: Carvedilol, transdermal, chemical enhancers, Percutaneous Absorption.


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