Abstract
Background: Controlled transdermal delivery system for vildagliptin is potentially useful in improving the clinical efficacy and reducing the incidence of adverse side effects. The objective of this study was to develop an adhesive transdermal system for the delivery of vildagliptin.
Methods: Vildagliptin-incorporated adhesive patches (P1-P10) were formulated on a polyester-release liner, and laminated with polyethylene-backing membrane. Optimization of the patches was done by conducting ex vivo permeation studies. The effects of varying the type of pressure-sensitive adhesive, drug concentration and chemical enhancer, on the flux was studied. Optimized patch (P8) was prepared with the use of Duro-Tak 87-2516 as pressure-sensitive adhesive, drug concentration of 10% (w/w) and isopropyl myristate as permeation enhancer. In vivo pharmacokinetic parameters were determined in male wistar rats for optimized and control patch and Tmax, Cmax and AUC0-α values were compared.
Results: Tmax values were equal for the optimized patches and the control (6 h), while Cmax values was much higher for optimized patches. Vildagliptin was detected in the plasma in first hour of sampling. The AUC0-α value of the optimized patches was 147.5 ± 28.44 ng.h/ml, and this was ~5 folds higher relative to control.
Conclusion: These results suggest that transdermal delivery system seems to be promising alternative method for the use of vildagliptin in the management of type 2 diabetes.
Keywords: Diabetes mellitus, patch, pharmacokinetics, rats, transdermal, vildagliptin.
Graphical Abstract
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