IMPROVEMENT OF WATER SOLUBILITY AND IN VITRO DISSOLUTION RATE OF DEFLAZACORT BY COMPLEXATION WITH Β-CYCLODEXTRIN THROUGH FREEZE DRYING PROCESS

Abstract

Deflazacort is a poorly water-soluble drug and is practically insoluble in water. The objective of this study was to improve the solubility of deflazacort by using as solubility enhancer β-cyclodextrin and also to study the effect of the water-soluble polymer PEG 4000 on solubility of the deflazacort:β-cyclodextrin binary system. The inclusion complexes of deflazacort with β-cyclodextrin in 1:1 w/w, 1:2 w/w and 1:3 w/w proportions were prepared by kneading, microwave irradiation and freeze-drying techniques. The in vitro dissolution study showed improved dissolution rate for deflazacort for freeze-dried binary deflazacort: β-cyclodextrin 1:2 w/w complex, as compared to ternary deflazacort:β-cyclodextrin: PEG 6000 1:2 w/w complexes, plain deflazacort, physical mixtures and complexes prepared by kneading and microwave technique. This was confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, powder x-ray diffraction study, scanning electron microscopy and 1 H nuclear magnetic resonance spectroscopy study. Thus, deflazacort:β-cyclodextrin complex with improved solubility was successfully developed using freeze drying technique.