DEVELOPMENT, EVALUATION AND IN-VIVO ASSESSMENT OF FENOPROFEN CALCIUM-LOADED NANOPARTICLE-BASED TRANSDERMAL PATCHES

Background: The objectives of this study were to prepare and test fenoprofen calcium loaded nanoparticles for transdermal patches and to study the preliminary dermal tolerability and in-vivo anti-inflammatory effect of optimized formulation. Methods: A total of six formulations (TP1–TP6) were prepared in the solvent-casting method with different amounts of hydroxypropyl methylcellulose (HPMC), Eudragit RLPO, Eudragit RSPO and ethyl cellulose. Physical and Mechanical properties, Drug Content, Moisture content, Water vapour transmission rate (WVTR) and in-vitro drug diffusion were evaluated on the patches. The optimized formulation was subjected to accelerated stability test at 75 ± 5%RH and temperature 40 ± 2°C for six months. The dermal irritation and anti-inflammatory activity were evaluated in the Wistar albino rat skin irritation test and carrageenan-induced paw oedema model, respectively. Results: Formulation TP5 exhibited the best overall performance with folding endurance of 245 ± 5.7 folds, tensile strength of 0.86 ± 0.019 kg/cm², elongation of 38.2 ± 1.3%, drug content of 98.2 ± 0.6%, moisture content of 3.9 ± 0.15%, and WVTR of 4.1 ± 0.21 g/m²/24 h. The cumulative drug diffusion was 97.1 ± 0.92% after 24 hours. The drug content in the accelerated stored samples was 95.8 ± 1.1% after 6 months with no change in appearance. The primary irritation index for TP5 was 0.17. At 24 hours, mean paw thickness was 5.72 ± 0.05 mm for TP5, 5.76 ± 0.04 mm for oral nanoparticles, and 5.86 ± 0.03 mm for the oral reference group. There was a significant reduction in paw thickness compared with the reference group in the case of TP5 and oral nanoparticles. Conclusion: Further skin permeation, pharmacokinetic, stability and safety studies of TP5 were warranted due to its promising formulation properties and initial in-vivo activity.