The Inclusion Complex of Allicin with Β-Cyclodextrin as A Drug-Delivery System for Enhanced Solubility in the Treatment of Breast Cancer

The goal of this study was to enhance the aqueous solubility, stability, and therapeutic efficacy of allicin, a bioactive organosulfur compound found in garlic (Allium species), through the formation of a β-cyclodextrin (β-CD) inclusion complex without altering the chemical structure of allicin. Allicin is widely recognized for its pharmacological potential but suffers from poor water solubility, instability, and strong odor, which limit its bioavailability and therapeutic application. In this study, β-CD was used to form an inclusion complex with allicin using the co-precipitation method. Various ratios of allicin to β-CD (1:1, 1:2, and 2:1) were evaluated, with the optimal complex obtained at a 1:1 weight ratio. The optimized complex achieved a drug loading of 50% ± 0.63 and an entrapment efficiency of 86.1% ± 0.37. Characterization of the inclusion complex was carried out using Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), and scanning electron microscopy (SEM), confirming successful complex formation. Solubility studies demonstrated a significant increase in allicin's solubility from 0.52±0.03 mg/ml to 4.82±0.08 mg/ml after complexation. In-vitro dissolution testing revealed an improved release profile, with the inclusion complex achieving 94.10±0.05 % release within 2 hours, compared to 48.79±0.16 % for free allicin. Additionally, cytotoxicity studies against the MCF-7 breast cancer cell line showed that the allicin/β-CD complex exhibited a higher inhibition rate (147.54± 2.10 μg/ml) compared to allicin alone (69.66±8.58 μg/ml). These results indicate that β-cyclodextrin inclusion complexation is a promising strategy for enhancing the solubility, stability, and therapeutic performance of allicin.