Experimental Design for the Optimization of Nanoscale Solid Lipid Particles Containing Rasagiline Mesylate

Abstract

Background: The objective of this investigation was to design and optimize the fabrication of Rasagiline mesylate loaded nanoscale solid lipid particles composed with stearic acid as lipid matrix by microemulsion technique. Rasagiline (N-propargyl- 1-R-aminoindan) mesylate (RM) is a potent, selective, irreversible inhibitors of monoamine oxidase-B, propargylaminebased drug. It has been explored in the treatment of Parkinson disease. Nanoscale solid lipid particles are the exploited carrier system for targeted drug delivery in a controlled manner. Method: The Plackett-Burman design was successfully employed for the optimization of nanoscale solid lipid particles containing Rasagiline mesylate. The influence of independent variables studied were lipid, surfactant and co-surfactant concentration, volume of aqueous phase, magnetic stirring rate, probe sonicator duration, volume of beaker used and volume of cold aqueous phase. The dependent variables, namely average particle size, span, surface area and polydispersity index of the formulated Rasagiline mesylate loaded solid lipid nanoparticles. Results: The experiments were carried out according to 12 runs involving 8 independent variables (higher and lower levels) employing Plackett-Burman design. The Rasagiline mesylate-loaded solid lipid nanoparticles were characterized by average mean particle size, span, surface area and polydispersity index and it results were 169 nm, 0.821, 52.4 m 2 g -1 and 0.310, respectively. The morphological evaluation of optimal Rasagiline mesylate loaded solid lipid nanoparticles was found to be monodisperse, uniform size and quasispherical shape with smooth surface by transmission electron microscopy (TEM). The selected area electron diffraction (SAED) indicated the formulation was not in an amorphous form but in a crystalline state. Conclusion: The experimental results were good correlated with predicted data analysed by Plackett-Burman statistical method. Key words: Plackett-Burman, Rasagiline mesylate, Ransmission electron microscopy, Selected area electron diffraction, Solid lipid nanoparticles.