Formuation, Statistical Optimization and In-Vitro Evaluation of Antihypertensive Losartan Potassium Nanoparticles

Abstract

Present study is focused to formulate, optimize and evaluate polymeric nanoparticles (PNPs) of losartan potassium, to overcome its shortcomings of moderate bioavailability, short terminal half life and potential adverse effects. Drug loaded nanoparticles were prepared by emulsification method followed by solvent evaporation using the polymer ethyl cellulose and PVA as stabilizer. Total seventeen formulations were prepared and analyzed by altering formulation and process variables like concentration of polymer and surfactant, sonication time. Optimization was based on two dependent variables, particle size and entrapment efficiency using design of experiment approach with box behnken design. Optimized nanoparticle formulation was evaluated for particle size, shape, entrapment efficiency and zeta potential. In-vitro drug diffusion studies were carried out to understand the drug release behavior. The optimized nanoparticle formulation was found to have the particle size of 423.4 nm, zeta potential -11.4 mV, and entrapment efficiency of 85.57%. SEM analysis showed the smooth, spherical surface of the prepared nanoparticles. Cumulative drug release was 98.42% over a period of 12 hrs. The release pattern followed higuchi model with highest r² value of 0.935. Formulation was found to be stable during three months stability studies. Based on the results, the formulated nanoparticles were found to have the great potential for the sustained delivery of antihypertensive losartan potassium.