<p>Globally, breast cancer is one of the most widespread malignancies among women, posing a significant Healthcare challenge that necessitates a comprehensive treatment approach. This paper explores the potential of phytochemicals as therapeutic agents for breast cancer, focusing on their extraction processes, bioavailability challenges, and advancements in drug delivery systems. Phytochemicals, which originate from natural sources, exhibit remarkable bioactivity and can modulate various biochemical pathways involved in cancer progression, making them potential adjuncts or alternatives to conventional therapies. While over 100 phytochemicals with anticancer properties have been identified, only ten have progressed to clinical trials. This limited progress is largely due to challenges in identifying, extracting, and isolating bioactive compounds from crude extracts. Employing in silico approaches alongside advanced extraction technologies can significantly reduce the time required to identify and isolate the therapeutic compounds. However, the therapeutic application of phytochemicals remains constrained by issues such as low solubility, poor absorption, and inadequate tissue penetration. To overcome these limitations, innovative drug delivery systems—particularly nanoparticle-based technologies—are being developed to improve the solubility, bioavailability, and targeted delivery of these compounds. Leveraging advanced delivery methods and maximizing the therapeutic potential of plant-derived bioactive compounds could significantly contribute to the development of effective and sustainable breast cancer treatments.</p>