Development of Transdermal Delivery System of Vildagliptin and Its Comparison with Oral Therapy

Abstract

Purpose: The long term oral therapy of vildagliptin is associated with potential hepatotoxicity and low patient compliance. This study aims at development of a drug in adhesive transdermal patch system of vildagliptin using pressure sensitive acrylic polymers and compare the pharmacokinetics with oral therapy.Methods: The prospective of different chemical enhancers in improving the transport of vildagliptin was assessed ex vivo. In vivo permeation studies in rats were performed using patch system contain sodium lauryl sulfate as enhancer.Results: Drug solubility varied among adhesive bases tested and maximum value (15% w/w) observed with Duro-Tak 87-2510. Incorporation of chemical agents significantly improved the permeation of vildagliptin, but not to the same extent. The highest flux value of vildagliptin was obtained by the addition of sodium lauryl sulfate (22.96 ± 3.58 µg/cm2/h; P<0.0001), which is ~4 folds higher as compared to control. Pharmacokinetic profiles of vildagliptin were different for transdermal and oral delivery with significantly high bioavailability by transdermal delivery. The AUC0-α in transdermal delivery (1018.43 ± 79.56 ng.h/mL) was ~14 folds higher (P<0.0001) as compared to oral administration.Conclusion: The current study concludes that the fabricated drug in adhesive transdermal system could be employed for the effective delivery of vildagliptin.

Keywords: Transdermal; Adhesive; Vildagliptin; Enhancer; Flux; Pharmacokinetics