Formulation Optimization of Rosuvastatin Calcium-Loaded Solid Lipid Nanoparticles by 32 Full-Factorial Design

Kruti A. Dhoranwala, Pranav Shah and Shailesh Shah
 

Abstract

The present investigation was aimed at developing Rosuvastatin Calcium loaded solid lipid nanoparticles (SLNs). The SLNs were prepared using high pressure homogenization technique. Glyceryl monostearate (GMS) and Poloxamer 188 were employed as lipid carrier and surfactant respectively. A two factor, three level (32) full factorial design was applied to study the effect of independent variables i.e. amount of GMS (X1) and amount of Poloxamer 188 (X2) on dependent variables i.e. Particle size (Y1) and % entrapment efficiency (Y2). Particles size, % entrapment efficiency (%EE), zeta potential, drug content, in vitro drug release and particles morphology were evaluated for SLNs. Contour plots and response surface plots showed visual representation of relationship between the experimental responses (dependent variables) and the set of input (independent) variables. The adequacy of the regression model was verified by a check point analysis. The optimized batch (B10) contained 2.2 gm of GMS and 1% of Poloxamer 188. Batch B 10 exhibited mean particle size of 529.6 nm ± 6.36 nm; polydispersity index (PDI) of 0.306 ± 0.042; zeta potential of -31.88 mV ± (-2.50) mV and %EE of 48.90% ± 1.72%. The drug release experiments exhibited an initial rapid release followed by sustained release extended upto 36 h. Differential scanning calorimetry (DSC) studies showed that there was no chemical interaction between drug (Rosuvastatin Calcium) and lipid (GMS) whereas scanning electron microscopy (SEM) studies indicated that Rosuvastatin Calcium loaded SLNs are spherical, discrete and homogenous. Accelerated stability studies showed that there was no significant change occurring in the responses after storage for a total period of 3 months.

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