Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutics

The aim of this thesis is to formulate and evaluate lacidipine nano-dispersions to improve its aqueous solubility and enhance its oral bioavailability. Lacidipine nanosuspensions were prepared by solvent {u2013} antisolvent sonoprecipitation technique according to a three factor, three level Box-Behnken design. The independent variables were: stabilizer to drug ratio (A), sodium deoxy cholate percentage (B) and sonication time (C). Whereas, particle size (Y1), zeta potential (Y2), and polydispersity index (Y3) were chosen as dependent variables. Optimized lacidipine nanosuspension was obtained using the Design Expert® software. The optimum lyophilized lacidipine nanosuspension was evaluated regarding its particle size, zeta potential, polydispersity index, X-ray powder diffraction, differential scanning calorimetry, transmission electron microscopy, solubility in water and 0.1N HCl and in-vitro dissolution rate. Lacidipine polymeric micelles were prepared by thin film hydration technique according to a two factor, three level central composite face-centred design. The independent variables were: Pluronic to drug ratio (A) and Pluronic P123 percentage (B). Whereas, entrapment efficiency (Y1), particle size (PS) (Y2), and polydispersity index (PDI) (Y3) were chosen as dependent variables. Optimized lacidipine polymeric micelles formula was obtained using the Design Expert® software. The optimum lyophilized lacidipine polymeric micelles formula was evaluated regarding its entrapment efficiency, particle size, polydispersity index, Fourier-transform infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, solubility in water and 0.1N HCl and in-vitro dissolution rate. In-vivo study was performed to compare the pharmacokinetic parameters of lacidipine after the oral administration of lacidipine polymeric micelles and lacidipine oral suspension

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