ABSTRACT:
Valsartan is BCS Class II drug having poor bioavailability and used as an antihypertensive agent. Objective: The objective of the work is to improve the permeation of valsartan by incorporating solid lipid nanoparticles (SLN) of valsartan in the transdermal patch. Material: Valsartan, ethyl cellulose, compritol 888, tween 80, polyvinyl pyrrolidone. Method: 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. Result and Discussion: 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. Conclusion: Result of Ex-vivo study shows that the solid lipid nanoparticles can be successfully used as vehicle for improvement permeation of drug.