Abstract

SYNTHESIS AND EVALUATION OF TRANSDERMAL PERMEATION OF METAPROLOL ESTER PRODRUGS.

C. H. Prathyusha*, V. Divya Sai Jyothi*, P. Divya Bharghavi*, B. Abhilash and P. Srinivasa Babu

ABSTRACT

Metaprolol is a selective β1 receptor blocker medication used to treat high blood pressure and other heart related problems. It has a short half-life due to extensive first pass metabolism and hence oral & IV routes are ineffective & repetitive doses of the drug should be taken and thus, transdermal drug delivery is selected as an alternative route for Metaprolol administration. For transdermal drug delivery system Metaprolol tartarate and succinate salts cannot be used because of their low transdermal permeation and Metaprolol as such cannot be used because of its high water solubility and poor lipid solubility. Inadequate skin permeability is the main challenge encountered in the transdermal drug delivery and to solve this problem physical and chemical enhancement techniques are being developed. The purpose of the present investigation is to study the effect of esterification, on the transdermal delivery of metaprolol. Three ester prodrugs of metaprolol were synthesized, characterized by IR spectroscopy and studied for physicochemical properties like solubility and partition coefficient and in vitro permeation studies of using Franz diffusion cell at different donor concentrations (5, 10 and 20 mmol/l) using porcine skin.

Keywords: Metaprolol, transdermal drug delivery, partition coefficient, Invitro permeation, franz diffusion studies.