Formulation development and characterization of Lecarnidipine hydrochloride niosomal transdermal patches

Abstract

The bioavailability of Lercanidipine Hydrochloride (LCP) is about 44% and half-life of the drug is about 4.6 hours. LCP due to its low therapeutic dose range of 2.5 to 20mg and substantial biotransformation in liver becomes it ideal molecule in development of transdermal therapeutic system. The primary objective of the present research work was to develop Niosomal transdermal patch (NP) of Lecarnidipine. The LCP nanoparticles were prepared by solvent evaporation method and the optimized Nanoparticles formulation has shown 225nm particle size with a polydispersity index (PDI) of 0.120. LCP patches were prepared by incorporating nanoparticles dispersion, using varying concentrations of polymers HPMC E5, HPMC 5cps, HPMC 15cps, Carbopol 734 and Sodium alginate using solvent casting techniques and further optimized by central composite design(CCD) the effect of polymer on the various physico-chemical characteristics and in-vitro drug release studies, ex-vivo skin permeation studies is studied. On the basis of in-vitro drug release and ex-vivo skin permeation studies, the formulation containing (HPMC 15cps and HPMC 5cps) has shown sustained and extended drug release over a period of 24 hrs. Keywords: Lecarnidipine; Niosomes; Transdermal patch; Central composite Design, Controlled release; Bioavailability etc.