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Curcuminoids originating from turmeric roots are renowned for their diverse pharmacological applications, particularly as a natural anticancer agent. Unfortunately, harnessing the full potential of curcumin derivatives in cancer therapy has been impeded by its inherent limitations, specifically instabilities owing to poor solubility, leading to low systemic bioavailability under normal physiological circumstances. To circumvent this, a novel organic-based drug delivery system employing physically adsorbed β-cyclodextrin (βCD) as an excipient was developed in this study. This resulted in improved aqueous dispersion coupled with anticancer enhancements of tetrahydrocurcumin (THC) at a molar ratio of 2:1. Encapsulation of this agent was confirmed by physicochemical characterisation using UV-vis spectroscopy, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and both in vitro and in vivo approaches. Through the presence of an inclusion complex, a higher aqueous dispersion (65-fold) resulting in a higher drug content and an elevated release profile was achieved. Athymic nude (Nu/Nu) mice exposed to this treatment displayed improvements in tumour regression compared to stand-alone agents, consistent with in vitro cytotoxicity assays with an SI value > 10. The inclusion complex further enhanced apoptosis, as well as anti-migration and anti-invasion rates. Mechanistically, this formulation was consistent in terms of caspase 3 activation. Furthermore, the inclusion complex exhibited reduced systemic toxicity, including reduced inflammation in vital organs as examined by hematoxylin and eosin (H&E) staining. This study also revealed a notable sequential reduction in serum levels of tumour markers, including carcinoembryonic antigen (CEA) and mouse Cytochrome P450 1A2 (CYP1A2), correlating with a significant decrease in tumour bulk volume upon treatment commencement. These compelling findings highlight the potential of this formulation to empower insoluble or poorly soluble hydrophobic agents, thus offering promising prospects for their effective utilisation in colorectal cancer (CRC) chemotherapy., Competing Interests: All authors declare that there are no conflicts of interest., (Copyright: © 2024 Low et al. This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.)