Berberine, a secondary metabolite, basically an isoquinoline alkaloid, derived from various species of Berberis and Coptis has significant biochemical effects like anti-inflammatory and anti-cancerous at various sites of the human body. Its role is significant in ovarian cancer. As an anticancer agent, it can block the cell cycle, can hinder activity of topoisomerases, can upregulate the expression of proteins to activate apoptotic cascade in various cell lines. It can also inhibit metabolic process of tumor cells which leads to the death of tumor. Moreover, repopulation of tumor stem cells can also be inhibited by berberine therapy. Combined dose therapy enhances its efficacy against malignancy. However, poor absorption and efflux from digestive tract limit its benefit. This problem is overcome by the production of its derivatives or by the formulation of berberine Nano-carriers. Also, its specificity towards its target site is increased through Nano-formulation. So, this study explores the biochemical characteristics and effective chemotherapeutic pathways of berberine, also highlights the strategies that include using berberine in combination with other chemotherapeutic agents either to reduce toxic side effects or enhance their anticancer effects and determines the potential of various novel formulation approaches to enhance pharmacokinetics of berberine.