Analysing the Effect of Permeation Enhancers on the In Vitro Skin Permeability of Propranolol: A Mechanistic Study

Propranolol hydrochloride is a non-selective beta-adrenergic blocker. Due to extensive first pass metabolism, it shows variable bioavailability. Up to now, several researches has been conducted regarding its effect on wound healing. Hence, transdermal delivery of this drug could be helpful to overcom the first pass metabolism and delivery of the drug into skin. In this study, the effect of different permeation enhancers namely Isopropyl myristate, Labrafac, Labrafil, Olive oil and Plurol oleique on skin permeability of propranolol through rat skin has been analysed through a Franz cell and by evaluating the parameters like Jss, ERflux, ERD and ERp. The effect of enhancers on skin structure was studied by using FT-IR and DSC techniques. Enhancement mechanisms were evaluated through comparing FT-IR peak intensities for asymmetric and symmetric C-H stretching, ester C=O stretching and Amide peaks. Mean transition temperature (Tm) as well as their enthalpies (H) studied by DSC technique. It was shown that all the permeation enhancers improved permeability of the drug through rat skin. Among them, Labrafac had more effect on flux having ERflux value of 9.24 and plurol oleique had more effect on ERD having value of 13.99 due to the positive effects on skin lipid-protein structure while Isopropyl myristate has shown the least effect. According to the obtained results, the use of chemical permeation 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 propranolol.

Automated summary

In this study, the effect of different permeation enhancers on the skin permeability of propranolol was analyzed. It was shown that all the enhancers improved the permeability of the drug through rat skin. Labrafac had the greatest effect on flux, with an ERflux value of 9.24, while Plurol oleique had the greatest effect on ERD, with a value of 13.99. Chemical permeation enhancers can be considered as suitable excipients in transdermal delivery of propranolol due to their ability to change the skin structure and increase drug permeability.