Aqueous solubility and stability enhancement of astilbin through complexation with cyclodextrins.

Abstract

The complexation of astilbin with α-, β-, and γ-cyclodextrin (CD) was studied by phase solubility test and UV-vis spectral titration. Complexation with CDs gradually decreased the absorbance of astilbin at 291 nm and obviously increased its water solubility. The formation constant (K(a)) between astilbin and the three CDs was calculated. The stability of astilbin complexes increased in the order α-CD < γ-CD < β-CD, attributed to the CDs' cavity size. Temperature studies showed that the K(a) value decreased along with the rise of temperature. The negative values of enthalpy and entropy during complexation indicated that the complexation process was enthalpy-controlled. In alkaline medium isomerization and decomposition of astilbin were found; however, the addition of CDs significantly improved its stability through complexation. The solubility of astilbin in β-CD microcapsules prepared by the freeze-drying method was enhanced by 122.1-fold, and its dissolution profile was improved.