Abstract
APPLICATION OF FACTORIAL DESIGN TO FORMULATE AND OPTIMIZE LOSARTAN POTASSIUM- LOADED SOLID LIPID NANOPARTICLES

Mohamed El-Araby*, Sanaa A. El-Gizawy, Esmat A. Zein El Dein and Mohamed A. Osman

ABSTRACT

Losartan Potassium (LP) belongs to class III in biopharmaceutics classification system with antihypertensive activity. The aim of this study is to design Losartan Potassium loaded Solid lipid nanoparticles (LP-SLNs) and to optimize on their physio-chemical properties including particle size (PS), entrapment efficiency (%EE), zeta potential (ZP) and in-vitro release of drug. Losartan Potassium loaded solid lipid nanoparticles (LP-SLNs) were prepared by means of a w/o/w double emulsion solvent evaporation technique employing stearic acid alone or mixture of stearic acid and Geleolâ„¢ as a lipid matrix. A (23) non-randomized full factorial design was adopted to optimize LP-SLNs physicochemical properties. Three independent parameters were selected in this design including the lipid type, the concentration of polyvinyl alcohol (%w/v) and the amount of lipid (mg). The impacts of these parameters on particle size (PS), entrapment efficiency (%EE), zeta potential (ZP) and in-vitro release of drug were inspected. The designed preparations of LP-SLNs possessed a spherical shape with a particle size in the range of 294 nm to 671 nm and a negative zeta potential range from -18.04 to -8.02 mV. The % entrapment efficiency of LP-SLNs formulations were found to be in the range of 20.18 to 32.19. Fourier Transformation Infrared Spectroscopy (FTIR) revealed no possible interactions between LP and other additives while differential scanning calorimetric (DSC) manifested transformation of LP from crystalline to amorphous state in SLNs formulation. Stability studies of the chosen freeze dried LP-SLNs formulations showed a high stability during a period of three months.

Keywords: Solid Lipid Nanoparticles, Losartan Potassium, factorial design, stearic acid, Geleolâ„¢.


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