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Cancer continues to pose a worldwide health concern, requiring breakthrough therapeutic approaches that are both efficacious and minimally intrusive. Berberine, a natural isoquinoline alkaloid, has attracted considerable interest due to its various pharmacological features, particularly its strong anticancer effects. Nonetheless, its clinical application has been impeded by inadequate bioavailability, rapid metabolism, and systemic elimination. Recent breakthroughs in nanotechnology have mitigated these issues by creating BBR nanoparticles (BBR NPs), which provide increased solubility, precise delivery, and higher therapeutic efficacy. This paper extensively examines BBR and its nanoparticle forms for cancer treatment. The mechanisms of action, including apoptosis induction, tumour angiogenesis inhibition, antimetastatic effects, and oxidative stress modulation, are thoroughly examined. Essential synthesis approaches for BBR nanoparticles, including chemical reduction, green synthesis, and encapsulation in nanocarriers, are discussed together with their characterization methodologies. The report emphasizes comparative studies that illustrate the enhanced antitumor efficacy of BBR nanoparticles compared to free BBR in preclinical settings. Notwithstanding encouraging results, nanoparticle stability, scalability, and regulatory obstacles must be resolved for effective clinical translation. Future directions are examined, encompassing advancements in nanoparticle design and their prospective incorporation into personalized oncology. This review highlights the transforming potential of BBR and its nanoformulations as a novel therapeutic approach in cancer treatment.
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