β-Cyclodextrin-based inclusion complexes and nanocomposites of rivaroxaban for solubility enhancement
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Rivaroxaban (RIV) is an oral anticoagulant used in the prevention of venous thromboembolism in adult patients after total hip replacement or total knee replacement surgery. It is practically insoluble in water and buffer systems (pH 3–9). The present study was aimed to investigate the β-CD-based inclusion complexes and nanocomposites of rivaroxaban (RIV) for solubility and dissolution enhancement. A novel solubility enhancement approach of inclusion complexation of RIV with β-CD using spray drying method combined with high pressure homogenization as a particle engineering method was used. Change in crystallinity of RIV nanocomposites was assessed by DSC and PXRD. The interaction of drug with β-CD was projected through 1H-NMR and FT-IR studies. Saturation solubility and in vitro dissolution study revealed a dramatic increase in solubility and dissolution of RIV, respectively. Thus, spray-dried β-CD-based nanocomposites could be an innovative approach for solubility and dissolution enhancement of RIV.
The authors are thankful to Symed Laboratories, Hyderabad, India and Gangwal Chemicals, Mumbai, India, respectively for gift sample of Rivaroxaban and β-cyclodextrin, respectively.
This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors.
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