Complexation of Haloperidol with a Water‐soluble β‐Cyclodextrin Polymer: Characterization of the Inclusion Complex in Solid State and in Aqueous Solution

Abstract

Haloperidol, a highly hydrophobic drug, was complexed with a β-cyclodextrin polymer. Its solubility was increased 24 times in the presence of a 10-fold excess of this polymer. The stability constant of the complex was calculated from the phase solubility technique. Differential scanning calorimetry was used to confirm the complexation in solid state and 1H NMR in aqueous solution. The enthalpy and the entropy of the system were calculated by monitoring the isothermic solubility line at four different temperatures, indicating that the complexation of haloperidol with this particular β-cyclodextrin polymer is a favourable procedure. These findings could result in a new, non-acidic water soluble formulation of haloperidol.