Transdermal Permeation Enhancement of Valsartan Using Solid Lipid Nanoparticles

Valsartan is BCS Class II drug having poor bioavailability and used as an antihypertensive agent.

The objective of the work is to improve the permeation of valsartan by incorporating solid lipid nanoparticles (SLN) of valsartan in the transdermal patch.

Valsartan, ethyl cellulose, compritol 888, tween 80, polyvinyl pyrrolidone.

Valsartan loaded solid lipid nanoparticles (VAL-SLN) were prepared by pre-emulsion sonication method and spray dried to improve the handling, and stability. Scanning Electron Microscopy (SEM) of optimized formulations was carried out to determine morphology of VAL-SLN. Valsartan loaded solid lipid nanoparticles (VAL-SLN) were incorporated into ethyl cellulose (EC) and polyvinyl pyrrolidone (PVP) matrix patch prepared by solvent evaporation method. This patch was evaluated for thickness, weight variation, folding endurance. Ex-vivo skin permeation on rat skin was studied.

The VAL-SLN with particle size (248.87 nm) and entrapment 98.23± 1.08%. was prepared and obtained in spray dried form. FTIR indicated absence of any chemical interaction between valsartan and the lipids. The DSC thermogram showed an endotherm shift in VAL-SLN compared to that of lipid and was different from that of drug, The VAL-SLN formulations showed spherical shape with smooth and non porous surface in SEM. Ex-vivo skin permeation studies on plain valsartan and VAL-SLN containing patches showed flux (17.33±0.7 μg/hrs/cm²) and (42.23±3.1 μg/hrs/cm²) respectively.

Result of Ex-vivo study shows that the solid lipid nanoparticles can be successfully used as vehicle for improvement permeation of drug.