European Journal of Biomedical and Pharmaceutical Sciences

DESIGN DEVELOPMENT AND EVALUATION OF TRANSDERMAL DRUG DELIVERY SYSTEM OF EPROSARTAN MESYLATE

Shinkar Dattatraya Manohar*, Pandya Dimple Bhupendra, Saudagar Ravindra Bhanudas

ABSTRACT

Objective: Transdermal drug delivery systems are polymeric patches containing dissolved or dispersed drugs that deliver therapeutic agents at a constant rate to the human body. Eprosartan mesylate, a BCS class II drug with low solubility and high permeability has oral bioavailability of only 13% which is limited due to its poor aqueous solubility. Hence the objective was to develop transdermal patch of Eprosartan mesylate to enhance its bioavailability and to develop sustained release formulation of EPM to deliver drug for 24 hrs. Method: Matrix type transdermal patches containing Eprosartan mesylate were prepared by solvent casting method with different quantities of hydrophilic (Hydroxy propyl methyl cellulose) and hydrophobic (Eudragit RS 100) polymeric system and Dibutylphthalate and dimethyl sulfoxide as plasticizer and penetration enhancer respectively. All the patches were optimized according to 32 factorial design. The transdermal patches were evaluated for their physicochemical properties such as thickness, weight uniformity, percent moisture absorption, percent moisture loss, folding endurance, tensile strength, percent elongation, water vapour permeation, surface pH, drug content uniformity, in vitro permeation study, skin irritation test and stability study. Result: FTIR and DSC studies were carried out which indicated no interaction between drug and polymers. In vitro drug permeation study reveals F8 formulation batch as optimized formulation with 94.00% drug release for 24 hrs. Permeation flux and permeability coefficient were found to be maximum for optimized batch. Drug release kinetics were found to follow first order release mechanism. Skin irritation studies on rat skin revealed patch to be non-irritant. The formulation was found to be stable for period of three months. Conclusion: Eprosartan can thus be formulated in the form of transdermal patch for effective delivery of drug via transdermal route and enhance bioavailability of the same.

Keywords: Transdermal patches, transdermal drug delivery system, Eprosartan mesylate, HPMC E15, Eudragit RS100.