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Feasbility of Transdermal Transport of Atenolol by Combination of Iotophoresis and Oleic Acid Pretreatment
Atenolol has a low oral bioavailability and a short elimination half-life. Therefore, alternative delivery system isimportant. Transdermal iotophoresis i.e. a systemic drug delivery via the skin, implementing a low intensity of electrical current, is one attractive candidate. This study evaluated feasibility of atenolol transdermal transport when lontophoresis was applied after enhancer pretreatment. There were 4 formulas prepared; 2 implemeneted lontrophoresis for 3 hours (current density: 0.25 mA/cm2 ) while the others did not use lontophoresis. The enhancer ws oleic acid (5 or 10% as a mixture in propylence glycol) with duration of pretreasment of one hour. Transport was evaluated based on the diffusion studies across the fresh rat skin in a static-vertical diffusion system. Data were analyzed based on the numeric convolution method to obtain simulated plasma concentration (CP) orifiles as well as area under the curve (AUC) of Cp profiles. Based on the simulated Cp, the best transport wasc achieved in Formula 3, where iontophoresis was performed across the skin, pretreated with 5% oleic acid. The values of simulated Cp indicated achievement of thereapeutics level of atenolol, sugesting the feasibility of the atenalol delivery by iontophoresis
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