In vitro and in vivo evaluation of a novel testosterone transdermal delivery system (TTDS) using palm oil base

Objective (s): Transdermal preparations for testosterone are becoming popular because of their unique advantages such as avoidance of first-pass effect, convenience, improved bioavailability, and reduction of systemic side effects. A novel testosterone transdermal delivery system (TDDS) was developed using a palm oil base called HAMINTM (a commercial product) and tested using in vitro and in vivo skin permeability test methods. Materials and Methods: The physical characteristics of the formulation such as particle size and viscosity were determined by using Franz diffusion cell and Brookfield viscometer, respectively. In vivo skin permeability test was performed on healthy rabbits through the skin. Testosterone in serum was analyzed using the validated Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS) technique. Results:  In vitro study showed that the cumulative amount of testosterone diffused was between ۴۰ to ۱۴۰۰ ngcm-² over a period of five hr after application of TDDS through the artificial Strat-M™ membrane. In the in vivo rabbit skin permeability test, the results indicated that testosterone was well absorbed with a mean Cmax and Tmax of ۶۰.۹۴ ngml-۱ and ۲.۲۹ hr after application of TDDS while no increase was observed in placebo treatment. Particle size analysis ranged from ۷۹.۴ nm to ۶۳۰.۰ nm for placebo and ۹۷ to ۷۷۴.۰ nm for TDDS. Conclusion: The formulation was successfully prepared using HAMINTM, which has demonstrated great potential for topical delivery of testosterone.

Keywords:

HAMINTM , Skin permeation , Testosterone , Transdermal delivery- system