New Approach for Pre-formulation of an Oral Cyclosporine

Development of new oral cyclosporine formulation using cyclodextrin tetrapolymer (Pαβγ-CD) in attempt to enhance its stability and dissolution rate.Two spray-dried dispersion formulations containing poorly water-soluble cyclosporine (CsA) were prepared with cyclodextrin tetrapolymer in water (FH2O) and ethanol (FEOH) then characterized by scanning electron microscopy, powder X-ray diffraction, particle size distribution, circular dichroism and nuclear magnetic resonance (NMR) along with the dissolution study which was compared to Neoral® and Sandimmune®. The physicochemical characterization studies showed an interaction between cyclosporine and P-αβγ-CD without secondary structure changes of cyclosporine. The order of cyclosporine release was as follows: (FH2O) = Neoral® ˃ (FEOH) ˃ Sandimmune®. The results could be explained by hydrophylisation and absence of crystallinity of cyclosporine. In conclusion, FH2O formulation revealed similar dissolution profile as Neoral® and better than Sandimmune®.