Abstract
Sitagliptin is a dipeptidyl peptidase 4-(DPP-4) inhibitor with glucose controlling capabilities that was effectively used for treating diabetes in the past. However, the oral administration of this drug caused such severe side effects that it was removed from the market. In the present study, Sitagliptin was formulated in a gel-type reservoir on a transdermal patch device, optimized by a mathematical simulation methodology, and experimentally validated in vitro using a Franz Cell apparatus. The mathematical model determined optimal design parameters which included 1% w/w acellulose as drug reservoir, transdermal patch rate control membranes, 1.25 mM initial drug concentration, 2 mL initial volume, and 4.52 cm2 patch area. This optimized reservoir formulation was then fabricated in the transdermal patch system and tested using Franz Cell to validate the simulation. The experimental results from the fabricated transdermal patch system indicated that Sitagliptin can be formulated in a patch to achieve the target effective plasma drug concentration in less than one hour and is able to sustain glucose control for over 24 hours.
Citation
Griffin JD, Colón S, Gray D, Overton B and Wang B. Design and Development of a Novel Sitagliptin-Loaded Transdermal Patch for Diabetes Treatment. SM J Biomed Eng. 2017; 3(4): 1022s.