Research Article: Enhancing Ezetimibe Anticancer Activity Through Development of Drug Nano-Micelles Formulations: A Promising Strategy Supported by Molecular Docking
Abstract:
Cancer remains a global health concern and a leading cause of mortality worldwide. The development of effective therapies for combating cancer is a critical area of research, necessitating the exploration of novel drug candidates and repurposing existing medications. Ezetimibe is primarily known for its role as an inhibitor of intestinal cholesterol absorption through its interaction with the Niemann-Pick C-like (NPCL) transporter., However, emerging preclinical and clinical data have suggested that ezetimibe may exhibit pleiotropic effects beyond its cholesterol-lowering activity, including potential anticancer properties. Recent in vitro and in vivo studies have demonstrated that ezetimibe exerts inhibitory effects on cancer cell proliferation, migration, and invasion. Moreover, it has been observed that ezetimibe can induce apoptosis, arrest the cell cycle, and inhibit angiogenesis in various cancer models., These findings indicate a potential role for ezetimibe as an adjuvant therapy or a standalone treatment option in cancer management. On the other hand, ezetimibe is characterized by its poor aqueous solubility (. mg/mL) and low bioavailability. The drug undergoes significant metabolism in the intestine and liver before entering systemic circulation. Its bioavailability was reported to be around –% due to extensive first-pass metabolism. To enhance its solubility and bioavailability, various nanoformulations of ezetimibe have been investigated. Nanoformulations aim to improve drug delivery, absorption, and efficacy. Nanosuspensions, nanoemulsions, lipid-based nanoparticles, and polymeric nanoparticles, made from biodegradable polymers, such as poly(lactic-co-glycolic acid) or chitosan, have been utilized to overcome ezetimibe limitations or drawbacks associated with the drug. Although these nanoformulations of ezetimibe may have addressed certain limitations, there may still be a demand to enhance the overall efficacy of ezetimibe.
Introduction:
Cancer remains a global health concern and a leading cause of mortality worldwide. The development of effective therapies for combating cancer is a critical area of research, necessitating the exploration of novel drug candidates and repurposing existing medications. Ezetimibe is primarily known for its role as an inhibitor of intestinal cholesterol absorption through its interaction with the Niemann-Pick C-like (NPCL) transporter. , However, emerging preclinical and clinical data have suggested that ezetimibe may…
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