Preparation and Characterization of Ivabradine HCl Transfersomes for Enhanced Transdermal Delivery

Abstract

Ivabradine HCl (IVB) is used in treatment of stable angina pectoris. The aim of the work was to prepare a once daily transdermal film of transfersomes loaded IVB. Transfersomes were prepared by modified ethanol injection method using three formulation factors namely: surfactant type, drug: phospholipid ratio and surfactant: phospholipid ratio. The transfersomes were characterized for entrapment efficiency, particle size, zeta potential, in vitro drug release, optical and transmission electron microscopy imaging, differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The best transfersomes showed optimal properties as well as pure drug were further formulated in transdermal film and characterized for content uniformity, folding endurance, weight and thickness, moisture content, moisture uptake, tensile strength and permeation through excised ear rabbit skin. Pharmacokinetic parameters of transfersomes incorporated film were compared with oral solution of the same drug dose. A maximum of about 82.03% entrapment efficiency, size of 206.7 nm, zeta potential of −88.3 Mv and 66.7% of drug release after 24 h were obtained from sodium lauryl sulphate based transfersomes at drug: phospholipid and surfactant: phospholipid ratio of 1:20 and 75:25 w/w, respectively. Films contained IVB transfersomes exhibited improved permeability and skin retention when compared with pure drug as well as enhanced pharmacokinetic parameters.