Preparation and in vitro–in vivo evaluation of QbD based acemetacin loaded transdermal patch formulations for rheumatic diseases

Abstract

This research aimed to develop patches for transdermal delivery of acemetacin, which can be used to treat rheumatic diseasesand to determine their potential use. Patches were successfully created by solvent casting method using hydroxypropyl methylcellulose, propylene glycol, polyethylene glycol 400, tween 80, and dimethyl sulfoxide. Prepared patches were found using the Design of Experiments (DoE) method within the Quality by Design (QbD) approach. F1-ACM with a thickness of 0.1 ± 0.0 cm, a weight of 43.33 ± 6.29 mg, pH of 4.99 ± 0.24, moisture content of 18.33 ± 2.98%, a tensile strength of 9.196 ± 0.441 Mpa, elongation at break of 28.722 ± 0.803% and drug content of 100% was chosen as ideal formulation. 89.7% of ACM from F1-ACM was released in 5 min. F1-ACM significantly (p < 0.05) increased the response latency to the thermal stimulus at 90th (3.071 ± 0.517) and 120th (3.87 ± 0.332) min in the hot plate test. In the tail-flick experiment, F1-ACM significantly (p < 0.05) increased the reaction delay against heat stimuli at 90th (3.016 ± 0.695), 120th (2.884 ± 0.851), and 180th (2.893 ± 0.932) min. F1-ACM patch significantly (p < 0.001) inhibited paw edema formation at 1, 2, 3, 4, and 5 h after induction of inflammation as compared to the control group. Therefore, this formulation can be employed more efficiently for rheumatic disease.