PALBOCICLIB LOADED SOLID LIPID NANOPARTICLES BY BOX-BEHNKEN DESIGN: SOLUBILITY ENHANCEMENT

The purpose of the present study was to optimize palbociclib-loaded solid lipid nanoparticles (SLNs) by evaluating the relationship between design factors and experimental data. A three-factor, three-level Box-Behnken design (BBD) was used for the optimization procedure, choosing the amount of tricapric, cremophor RH40 and soy lecithin, as independent variables. The chosen dependent variables were particle size, entrapment efficiency, and % cumulative drug released. The generated polynomial equations and response surface plots were used to relate the dependent and independent variables. The optimal nanoparticles were formulated with 08%tricapric, 09% cremophor RH40, and 6% soy lecithin. Three formulations were prepared according to these levels and found that the observed responses were close to the predicted values of the optimized formulation. The formulation PF13 was chosen for characterization as it displayed minimum particle size (103 nm), PI of 0.47, the zeta potential of -16 mV, maximum drug release of 98% in 12h. Fourier transform infrared spectroscopy (FT-IR) study indicated that the drug was entrapped in nanoparticles with no significant interaction between drug and excipients used. The optimized formulation showed a sustained zero-order release which followed the Peppas model. The formulation was stable when stored according to ICH guidelines for 6 months.