Preparation, characterization and permeation studies of a nanovesicular system containing diclofenac for transdermal delivery.

CONTEXT

Transdermal formulations contain permeation enhancer which causes skin damage. Ceramide 2 is natural lipid found in stratum corneum (SC).

OBJECTIVE

Drug-loaded nanovesicles of ceramide-2, cholesterol, palmitic acid, cholesteryl sulfate were formulated and analyzed for physical and biological properties. Diclofenac was used as a model drug.

MATERIALS AND METHOD

The vesicles were prepared using the film hydration method and characterized for physical parameters, in vitro drug release, accelerated stability studies and formulated into gel. Respective gels were compared with a commercial formulation (CEG) and plain carbopol gel (CG) containing drug for ex vivo, in vivo drug permeation and anti-inflammatory activity.

RESULTS

The vesicles were stable with optimum physical parameters. DCG-1 showed 92.89% in vitro drug release. Ceramide vesicles showed drug release between 18 and 25 μg/cm(2) whereas CG and CEG released 0.33 and 1.35 μg/cm(2) drug, respectively. DCG-1 and CEG showed corresponding Cmax at 6 and 4 h, respectively. DCG-1 showed six times AUC than CEG. DCG-1 inhibited edema by 86.37% by 4th hour of application.

DISCUSSION

The presence of ceramide 2 specifically promotes the drug permeation through SC and dermis and also contribute towards stability and non-irritancy.

CONCLUSION

The composition of the nanovesicle played an important role in physical properties and drug permeation.