Optimizing Transdermal Patch Formulation for Enhanced Delivery of Rivaroxaban: A Comprehensive Design of Experiments Approach

Abstract

Objective: To optimize Trans Dermal Patches (TDPs) of rivaroxaban using Poly Vinyl Pyrrolidone (PVP K30) and Hydroxypropyl Methyl Cellulose E50(HPMC E50) as hydrophilic polymers, Propylene Glycol(PG) as a plasticizer, and permeation enhancer. Methods: TDPs were crafted using a solvent casting technique with a 2-level, 3-factor factorial design. These patches were assessed for thickness, folding endurance, in vitro drug release, drug content, and moisture uptake and loss. An 8-stage diffusion cell apparatus facilitated in vitro drug release testing. The independent variables were HPMC E50, PVP K30, and PG. The change in the concentration of these independent variables resulted in the optimization of the transdermal patch. The dependent variables were the thickness, folding endurance, and in vitro diffusion. Results: The patch thickness ranged from 0.311±0.3 to 0.334±0.6. Folding endurance ranged from 58±0.7 92±6. The in vitro drug release ranged from 52.36% to 95.58%. The percentage drug content ranged from 83.58±0.4 to 95.26±0.5. The percentage of moisture content absorbed ranged from 21.36±0.13% to 25.54±0.26%. The percentage of moisture lost ranged from 1.01% to 2.31%. Conclusion: PG increased the release of rivaroxaban because it permeated the membrane. HPMC E50 is highly soluble. Thus, rivaroxaban patches are potentially suitable transdermal drug delivery systems.