Physicochemical and Biological Studies of Inclusion Complex of Methotrexate with β‐Cyclodextrin

Abstract

Methotrexate forms an inclusion complex with β-cyclodextrin (β-CyD) by a neutralization method. The formation of the inclusion complex was studied by phase solubility, X-ray diffractometry, differential scanning calorimetry and infrared spectroscopy. The amino group of methotrexate interacted with the hydroxyl function of β-CyD on complexation. The in-vitro drug release from the complex in phosphate buffer, pH 7–2, was better than that of the plain drug and other preparations evaluated. The complex had better bioavailability and showed better antitumour efficacy than methotrexate alone.