Enhanced Solubility and Dissolution Rate of Raloxifene using Cycloencapsulation Technique

Abstract

The aim of this study was to improve the water solubility of raloxifene by complexing it with sulphobutylether beta cyclodextrin Inclusion complexation in aqueous solution and solid state was evaluated by the phase solubility diagram powder X ray diffractometer Fourier transform infrared spectroscopy nuclear magnetic resonance scanning electron microscopy hot stage microscopy and transmission electron microscopy The inclusion complex behavior of raloxifene and sulphobutylether beta cyclodextrin were examined by molecular modeling method The phase solubility diagram with sulphobutylether beta cyclodextrin was classified as AL type curve indicating the formation of stochiomatric inclusion complex The apparent solubility constants calculated from phase solubility diagram was M Aqueous solubility and dissolution studies indicated that the dissolution rates were remarkably increased in inclusion complex compared with the physical mixture and drug alone In conclusion inclusion complexation with sulphobutylether beta cyclodextrin is an easy approach to increase raloxifene solubility and dissolution rate which could have implications in its bioavailability considering it a Biopharmaceutical Classification System Class II drug