Formulation, Development, and Characterization of Tadalafil Ethosomes for Transdermal Delivery: In Vitro Evaluation of Ethosomes Pharmaceutical Potentia

Abstract

The present research purpose was to develop ethosomes for transdermal delivery of Tadalafil, a recently approved phosphodiesterase-5 (PDE5) inhibitor, indicated for the treatment of erectile dysfunction by using various concentrations of phospholipids and ethanol. FT-IR studies confirmed that there was no chemical interaction between drug and excipients used in the formulation. The prepared formulations were evaluated for their vesicle size, shape, surface morphology, entrapment efficiency and in vitro drug permeation study. The ethosomes were spherical and discrete in shape. The size of vesicle was found to be in the range and sensible for skin penetration. Ethosomes of average size of 148.3 μm with a spherical shape bearing smooth surface were observed by transmission electron microscopy and surface electron microscopy. The maximum entrapment of ethosomes was found to be 72.37±0.55. The ethosomes showed highest entrapment efficiency and rapidly penetrate through the skin because of tiny vesicular size.  The % Cumulative amount of drug permeated through the biological membrane was found to be in the range of 0.24±0.05to 0.45±0.09 mg/cm2. The highest drug release leads to the increase in the bioavailability which indicates that the ethosomes are advanced nanoparticles. The stability study carried out for the period of 45 days showed negligible changes at room temperature. The result of in vitro release and characterization studies revealed that Tadalafil ethosomal formulation can deliver the drug more efficiently than conventional dosage form with no first pass metabolism and for a prolonged period of time.