Abstract
Emodin is a naturally occurring anthraquinone derivative that has great potential for cancer treatment. However, its lipophilic nature and its extremely low water solubility limit its physiological activities and therapeutic applications. In order to enhance solubility and stability, inclusion complex formation with cyclodextrin (CDs) is a promising method of choice. Therefore, emodin/hydroxypropyl-β-cyclodextrin (emodin/HP-β-CD) inclusion complex was prepared by a freeze drying strategy and the interactions of emodin with HP-β-CD were investigated using 1H nuclear magnetic resonance spectroscopy, Powder X-ray diffraction, Fourier transformation-infrared spectroscopy, Scanning electron microscopy and phase solubility studies. All the characterization information demonstrated the formation of emodin/HP-β-CD complex. The inclusion complex had stoichiometry of 1:1 and the stability constant (Ks) was calculated to be 1758.3 ± 5.7 M−1. The results demonstrated that the water solubility of emodin was remarkably increased (79-fold) and the stability was also improved in the presence of HP-β-CD. Furthermore, in vitro cytotoxicity studies showed that emodin/HP-β-CD complex had better antitumor efficacy than emodin alone. The enhanced solubility, stability and anti-cancer activity suggests that these inclusion complexes can be further used as feasible water-insoluble anticancer agents carrier in pharmaceutical formulations.
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