Formulation and optimization of upadacitinib-loaded transdermal patches for rheumatoid arthritis with zero-order release kinetics

Shubham  Talole; Rahul Godge; Nikita  Tambe; Nikita  Mhase

doi:10.69857/joapr.v13i2.1037

Authors

Shubham Talole Department of Pharmaceutical Quality Assurance, Pravara Rural College of Pharmacy Pravaranagar
Rahul Godge Department of Pharmaceutical Quality Assurance, Pravara Rural College of Pharmacy, Pravaranagar
Nikita Tambe Department of Pharmaceutical Quality Assurance, Pravara Rural College of Pharmacy, Pravaranagar
Nikita Mhase Department of Pharmaceutical Quality Assurance, Pravara Rural College of Pharmacy, Pravaranagar

DOI:

https://doi.org/10.69857/joapr.v13i2.1037

Keywords:

Upadacitinib, Transdermal patch, Factorial design, Zero-order kinetics, PVP K30, HPMC K4M, JAK inhibitor

Abstract

Background: To develop and optimize Upadacitinib-loaded transdermal patches for rheumatoid arthritis treatment with improved patient compliance and sustained drug delivery. Methodology: Upadacitinib transdermal patches were formulated using a 3² factorial design approach with PVP K30 and HPMC K4M as key polymeric components. The patches were characterized for physicochemical, mechanical, and ex vivo permeation properties. Results and Discussion: The optimized formulation (SF8) exhibited excellent physicochemical characteristics, including high drug content (99.05 ± 0.83%), optimal mechanical properties with tensile strength of 0.912 kg/mm² and adhesion strength of 3.94 N. The ex vivo permeation reached 86.35% at 12h, with the flux of 102.91 μg/cm²/h following zero-order kinetics (R² = 0.9777). The experimental values closely matched predicted values with less than 2% error. Accelerated stability studies confirmed minimal changes in critical parameters over six months. Conclusion: The optimized Upadacitinib transdermal patch provides sustained drug delivery with zero-order release kinetics and excellent stability. This transdermal delivery system offers a promising alternative to oral therapy with potential advantages of improved patient compliance, reduced dosing frequency, and avoidance of first-pass metabolism for rheumatoid arthritis management

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