Study on synthesizing the complex of sorafenib with 2-hydroxypropyl-β-cyclodextrin to enhance the anticancer activity of the drug substance

Abstract

Abstract This study aims to synthesize inclusion complex derived from sorafenib (Sor) and hydroxypropyl-β-cyclodextrin (HPβCD) (denoted as [Sor-HPβCD]). The complex of Sor with HPβCD has been synthesized in a mixed solvent of H2O-DMSO, with a DMSO volume fraction of 80 %. The results of FTIR, DSC, and UV–Vis analysis have demonstrated the success of complex formation: the intensity of some characteristic peaks for the Sor binding decreased after complex formation, indicating that a part of the guest molecule has entered the cavity of the HPβCD molecule. This is further supported by the DSC analysis results, showing the transformation of the complex’s crystalline form to an amorphous form. The phase solubility diagram study also indicates that the solubility of Sor significantly increases, approximately 7 times higher than pure Sor, after complex formation. The results of the cell growth inhibition activity test in a water environment show that the complex inhibits the growth of Hep-G2 cells with an IC50 value of 62.4 μg/mL, while pure Sor does not exhibit activity as it is practically insoluble in water.