Abstract 2178: A novel injectable formulation of quercetin reliant on the ability of the drug to complex copper

Low levels of fruit and vegetable consumptions have been linked to increased risk of cancer. Quercetin is one of the most ubiquitous flavanoids found in fruits and vegetables and there is increasing evidence that points to the anti-cancer potential of quercetin. This flavanoid acts as a promoter of apoptosis by modulating apoptosis through Bcl-2, Akt-1, and/or NF-κB. In addition, quercetin also demonstrated promise when used in combination with approved chemotherapeutic agents such as cisplatin and irinotecan. However, quercetin has remained largely clinically irrelevant despite all the potential anti-cancer benefits noted in in vitro assays. This is due in part to the low bioavailability of the compound and its poor aqueous solubility (solubility 98% encapsulation efficiency. Compared to previous data on free quercetin, the liposomal formulation of quercetin shows a markedly improved pharmacokinetic profile. The formulation demonstrated a 10-fold increase in elimination half life and a 7-fold increase in AUC when compared to previously published studies with free quercetin. A novel liposomal formulation of quercetin has been generated and the resulting formulation resolved the solubility issues faced when considering the use of quercetin for studies attempting to define its therapeutic activity in various cancer models. Citation Format: Kent T. Chen, Malathi Anantha, Ada W.Y. Leung, Mohamed Wehbe, Brent Sutherland, Marcel B. Bally. A novel injectable formulation of quercetin reliant on the ability of the drug to complex copper. [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 2178.