Diclofenac Loaded Nanoparticles Fabricated with Biomaterial (Ceramide 2) for Transdermal Delivery

Objective: Solid lipid nano particles loaded with model drug Diclofenac sodium were formulated using a biomaterial (ceramide 2) and evaluated for physicochemical properties, in vitro/ex vivo permeation and pharmacokinetic/ pharmacodynamic studies. Methods: The SLNs were prepared using modified emulsion/solvent evaporation method and characterized for physical parameters, in vitro drug release, accelerated stability studies. Then SLNs were formulated into gels and compared with a commercial formulation (CEG) and carbopol gel containing plain drug (CG) for ex vivo, in vivo drug permeation and anti-inflammatory activity. Key findings: The SLNs were stable with optimum physical parameters. GN-3 and SN-3 gave highest in vitro drug release. CNG-3 has shown higher drug permeation (158.49 mu g/cm(2)) into receptor fluid in ex vivo permeation study in comparison to CEG (1.35 mu g/cm(2)). The enhancement ratio of CNG-3 was 43.249 (with respect to CG). CNG-3 has shown almost 8.5 times C-max then CEO at 4 hours. The AUC value of CNG-3 was 16 times than CEG whereas CNG-3 provided 99.81% edema inhibition in 6 hours. Conclusion: Physicochemical properties of major lipid component govern the characteristics and permeation profile of SLN. SLN made up of ceramide-2 showed good physical properties with acceptable stability. It also showed promising transdermal permeation.