Preparation and Evaluation of Silymarin β-cyclodextrin Molecular Inclusion Complexes

Abstract

Silymarin is a hepatoprotective agent, having poor water solubility and oral absorption of about 23 – 47%, leading to low bioavailability of the drug. The aim of the present study is to improve the solubility and dissolution rate and in turn the hepatoprotective activity of the drug, by formulating its inclusion complex with beta (β)-cyclodextrin, using different methods. The phase solubility analysis indicates the formation of 1:1 molar inclusion complex of the drug with beta cyclodextrin. Apparent stability constant for Silymarin (Kc) was 722 K-1 with β-cyclodextrin complex. The inclusion complexes were prepared by four different methods, namely, physical mixing, kneading, co-precipitation, and solvent evaporation. The prepared complexes were characterized using differential scanning colorimetry, scanning electron microscopy, and x-ray diffractometry. The inclusion complex prepared by the co-precipitation methods exhibits an overall best result, with respect to the formulation of sustained release formulations.