Transdermal Delivery of Bisoprolol Hemifumarate

Abstract

The aim of this study was to formulate and evaluate the administration of bisoprolol hemifumarate (BH) using transdermal delivery systems. The following formulae were prepared as a reservoir to be used in batch formulae. Gels: carbopol 934 and carbopol 940 (C.934 and C.940); each in three different concentrations was prepared. In addition, emulgels were prepared and thermo sensitive gels utilizing Pluronic F127 (P.F127). The physicochemical properties of the drug were characterized by determining the partition coefficients. Subsequently, the prepared formulae were evaluated according to their rheological properties, in vitro release using a USP dissolution tester, in vitro diffusion using Franz's diffusion cells and bioavailability (studied in albino rabbits). All the formulae were manifested as pseudoplastic flow with thixotropy. In general, the viscosity of the prepared formulae increased with increasing the polymer concentrations, and this led to a decline in the percentage of the drug released. From all the formulae that were tested, pluronic F127 gave the highest drug concentration in rabbits (The highest Cmax and the lowest Tmax) in comparison to the other formulae and the oral commercial formulae. So, transdermal application of 20 % (w/w) P.F127 gel containing 0.5% w/w BH can be a promising new dosage form for treatment hypertension and angina pectoris. The significant findings presented here encourage further studies.

KEY WORDS: Bisoprolol hemifumarate, transdermal delivery systems; diffusion test; release study, bioavailability study.