Preparation and Characterization of Polymeric and Adhesive Matrix Diffusional Transdermal Drug Delivery Device of Atenolol

INTRODUCTION: The age-old theory that imparted the status of “dead, impermeable barrier devoid of biological activity” to skin had already been challenged by the development of pioneering transdermal product, but a less than impressive commercial growth in this sector had raised some doubts about the feasibility of this route as an efficient device of drug delivery. The journey of transdermal research had commenced with a lots of enthusiasm, as it heralded the promise of noninvasive cutaneous application. The projected advantages were publicized so much that the target consumers were prepared to accept the product even if they were costlier alternatives to the conventional therapy. This acceptability factor had encouraged researchers and industries alike to take up challenging project in this particular area. For the last two decades, it remained an area of vital research interest, and data was generated for almost every available drugs. Transdermal dosage forms, though a costly alternative to the conventional formulations, are becoming popular because of some unique advantages. Controlled zero order absorption, simple administration mode and the option of easy removal in case of adverse manifestations make them particularly desirable in cardiovascular therapy. Nitroglycerine and Isosorbide dinitrate, the two antiischaemic drugs; and the Clonidine, an antihypertensive molecule, are being extensively used in the transdermal form. Studies that compared with the established dosage forms had shown that though patches were costlier than conventional prescription products they reduced the occurrence of hospitalization and diagnostic cost. Currently numbers of antihypertensive drugs are under investigation for transdermal administration. Antihypertensive is group of cardiovascular agents that had generated excitement amongst the transdermal scientists, specifically the β-adrenergic receptor antagonist. These drugs have a multiple utilities and are administered in hypertension, ischaemic heart disease including certain types of arrhythmias. Since antihypertensive suffer from the disadvantages of extensive first pass metabolism and variable bioavailability, they were considered ideal transdermal candidate. Atenolol, a β-adrenergic receptor antagonist, has been shown to be safe and effective in the treatment of patients with hypertension. It has a mean plasma halflife of 6 hrs and only 45% of the orally administered drug reaches the circulation due to hepatic metabolism. A model reported predicts that mean plasma Atenolol concentration of 43, 99 and 175 ng/ml are required to produce a 20%, 30%, and 40% reduction in blood pressure respectively. This concentration can be achieved by preparing matrix diffusion controlled transdermal drug delivery system. Atenolol, a The present study was aimed at the development of polymeric and adhesive matrix diffusional transdermal drug delivery system of Atenolol using various polymers. Specific strategies like use of penetration enhancers shall be employed to meet systematic requirement of drug. Different formulation variable shall be studied and optimized to achieve the desired release profile. In the present investigation, the influence of various grades and concentration of polymers were studied. Po lymer i c Matrix type transdermal patches containing Atenolol were prepared using different polymers such as Ethyl Vinyl Acetate, ERS100, ERL100, Ethyl Cellulose, Poly Vinyl Pyrollidone and Hydroxy propyl methyl cellulose. Study was carried out to formulate an elegant product exhibiting desired therapeutic performance, from a small and cute dosage form. Finally selected devices shall be evaluated for in vitro study using human live skin. The delivery device was subjected to accelerated stability study as per ICH guideline. Results of stability study suggested a shelf life of 82 weeks (polymeric matrix) an d 75 weeks (adhesive matrix) stored at room temperature.