Development of a new nanovesicle formulation as transdermal carrier: formulation, physicochemical characterization, permeation studies and anti-inflammatory activity.

CONTEXT

Ibuprofen is an important NSAID, however, it can cause GI disturbances when given orally, and employment of transdermal route will require permeation enhancer causing skin injury.

OBJECTIVE

Drug-loaded nanovesicles of ceramide-2, cholesterol, palmitic acid, and cholesteryl sulfate (ICVG) were formulated and analyzed for physicochemical and permeation properties.

MATERIALS AND METHOD

Vesicles were formulated using film hydration method and physicochemical parameters, in vitro drug release, and stability were assessed. Further, nanovesicle gels were evaluated against plain gel containing drug (CG) for ex vivo/in vivo drug permeation and anti-inflammatory activity.

RESULTS

The developed formulations showed optimal physicochemical profile and ICV-1 gave 97.24% drug release. Drug permeation was between 17.32 and 33.12 μg/cm(2) for ICVG formulations and 0.27 μg/cm(2) for CG. ICVG-1 and CG showed Cmax of 9.6 and 0.7 μg/ml at 8 and 4 h. ICVG-1 showed 19.9 times higher AUC than CG. Edema inhibition was 57.98% during initial hours by ICVG-1.

DISCUSSION

Ratio of ceramide 2 and palmitic acid plays a critical role in drug permeation through stratum corneum. The stability and protective effect of the formulations were due to ceramide content.

CONCLUSION

The composition has an important role in physicochemical properties and drug permeation thereby generating an optimum formulation.