New approach for pre-formulation of an oral cyclosporine,” Digest

Development of new oral cyclosporine formulation using cyclodextrin tetrapolymer (P-αβγ-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 (F H2O ) and ethanol (F EOH ) 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: (F H2O ) = Neoral® ˃ (F EOH ) ˃ Sandimmune®. The results could be explained by hydrophylisation and absence of crystallinity of cyclosporine. In conclusion, F H2O formulation revealed similar dissolution profile as Neoral® and better than Sandimmune®