Abstract
Background and aimLosartan, an anti hypertensive agent, is required to be administered for a long period and it is AT-1 receptor antagonist. Aim of present work was to develop the controlled release formulation, transdermal delivery of losartan because of poor oral bioavailability (33%) due to extensive first pass metabolism. MethodsMatrix type TDDS was designed using polymers, polymethylmethacrylate (PMMA) and ethyl cellulose (EC), dimethyl sulfoxide (DMSO) a penetration enhancer and PEG-400 as plasticizer. ResultsNon-sticky, tough patches were obtained. Physical characteristics like moisture content, folding endurance and drug content were satisfactory with high drug content (97%), and uniform weights. Thirteen formulations were prepared and tested for integrity and in vitro drug release studies were carried out on Franz diffusion cell using dialysis membrane. ConclusionsAmong 13 formulations, LP-11 was better with in vitro cumulative drug release-76.5% in 24 h. The order of release was found to be first order and the mechanism of drug release was found to be Higuchi diffusion mediated.
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