CHARACTERIZATION OF TRANSDERMAL DELIVERY OF NEFOPAM HYDROCHLORIDE UNDER IONTOPHORESIS

In vitro iontophoretic delivery of nefopam hydrochloride was conducted to study the effects initial drug concentration, pH, ionic strength and viscosity of the donor solutions on the transdermal flux through a hairless mouse skin. Stability of nefopam hydrochloride under the experimental conditions was investigated. Type of electrode, current intensity, electric voltage and electrode distance were evaluated. Appropriate conditions were selected to minimize the potential degradation problems of nefopam hydrochloride during iontophoresis. Results show that the silver/silver chloride electrode provides better drug stability than the platinum electrode. Higher current intensity resulted in faster transdermal flux and therefore better drug permeability. The increase in the drug permeability appears to be proportionally increased as the current intensity increases in the range of 0.253 to 1.265 mA/cm(2). The iontophoretic transdermal delivery of nefopam hydrochloride was observed to increase as the drug concentration in the donor site was increased until it's close to the equilibrium concentration. The optimum pH to achieve the best iontophoresis under constant current was determined to be at pH 3.0. This may be due to the highest available charge density of nefopam was achieved at this pH to provide the best conductance. A decrease in the iontophoretic transdermal flux was encountered as an increase in the solution ionic strength due to the increased competition of similar charged ions with the available current. The increase in the donor solution viscosity decreased the conductivity of the ions and hindered the transdermal flux of the drug under iontophoresis.