Celiprolol hydrochloride (CLH) is a novel third generation drug used for the treatment of hypertension. It is a hydrophilic compound that is incompletely absorbed from gastrointestinal tract and leads to dose dependant low oral bioavailability. This study was aimed to determine CLH permeability through isolated rat skin by the use of iontophoresis approach. Glickfeld diffusion cell was used for in-vitro permeation study. Anodal iontophoretic delivery composition was optimized by evaluating pH of the vehicle solution, concentration of NaCl, current density, type of current and drug concentration. Increasing the pH of alkaline borate buffer from 8 to 10 resulted in doubling of the iontophoretic flux of CLH. Maximum drug permeation was found in presence of 0.1 M NaCl, more or less amount of NaCl was found to decrease drug permeation from alkaline borate buffer solution. The drug permeation was 46.125 µg/cm2/hr and 32.557 µg/cm2/hr in presence of pulsed depolarized DC current and continuous DC current, respectively. With increasing current density, the drug permeation was increasing almost linearly. Concentration of drug was observed non significant factor in alkaline borate buffer containing NaCl. Drug permeated from human cadaver skin (415.118±6.72 µg/cm2) was found to be laser than isolated rat skin (501.293±6.47 µg/cm2) when optimized composition was studied for comparative in-vitro permeation.
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