Design and Evaluation of Solid Lipid Nanoparticle Loaded Transdermal Patch of Nisoldipine: In Vitro, Ex Vivo and In Vivo Evaluation

Abstract

The objective of the research work is to develop and evaluate the solid lipid nanoparticles (SLNs) loaded matrix type transdermal patch of Nisoldipine (NSD). SLN formulations were developed and evaluated for particle size, zeta potential, polydispersibility index, drug content, entrapment efficiency then optimized formulation was freeze dried and incorporated into a transdermal patch. The physicochemical interaction between Nisoldipine and polymer was examined by DSC (differential scanning calorimetry) and FTIR (Fourier Transform Infrared Spectroscopy). Prepared patches were measured for thickness, uniformity of weight, folding endurance, moisture content, moisture absorption. The in-vitro and ex-vivo permeation of the Nisoldipine of the patches was studied by Franz diffusion cells. In vivo bioavailability study was performed using male wistar rats for optimized formulation N6 and compared with reference tablet (Sular). Dynasan 114 lipid (N-D4, formulation) is found to produce SLNs with low size and high entrapment efficiency. SEM analysis showed non aggregated spherical particles. N6(Formulation) patch containing 8% citral showed 96.5% of drug release and higher flux with 2.17 enhancement ratio (ER). Relative bioavailability of the test formulation with respect to market formulation was considered to be 2.52. The SLN loaded transdermal patches of Nisoldipine were developed successfully. There was considerable increase in bioavailability of the test formulation (N6) when compared to the marketed formulation. The increase may be attributed to avoidance of first pass metabolism of Nisoldipine which occurs through oral administration.