Development And Evaluation Of Transdermal Films Loaded With Antihypertensive Drug

Abstract

Objective: The aim of the present study was to prepare and evaluate transdermal films of Metoprolol Tartrate (MT) using sodium alginate (SA) and xanthan gum (XG) as biopolymers to minimize adverse effects associated with oral administration. Methods: Transdermal films of MT with SA / XG by varying the blend ratios were prepared by  solution casting method.  FTIR and DSC were studied to assess any interaction between the drug and the polymers. Drug loaded films were evaluated for physicochemical characteristics such as physical appearance, thickness, weight uniformity, folding endurance, % moisture absorption studies, SEM analysis, drug content uniformity. Tensile strength, invitro diffusion was determined by Franz diffusion cell. In vitro skin permeation of optimized formulation was compared with that of MT conventional gel. The patches were tested for their potential to cause skin irritation in rats. Results: Thin, flexible, smooth and transparent films of MT were obtained with SA/XG blends. The FT-IR and DSC studies confirmed no interaction between the drug and polymers. SEM pictures clearly exhibited the homogeneous dispersion of MT in the transdermal films. Thickness, Tensile strength, folding endurance and % elongation were found to be uniform and reproducible. In vitro diffusion release studies revels effectiveness of optimized formulation when compared with the conventional gel. The highest flux and enhancement ratio for MT from the film (A3) was found to be 0.268 ± 0.041 mg/cm²/h & 8.37 mg/cm²/h respectively. The skin irritation study indicated that neither the polymer nor the drug caused any noticeable irritation. Conclusions: It could be concluded that the polymeric matrix-type transdermal films of biopolymer based transdermal films are potential vehicles for improved transdermal delivery of MT effective therapy.