Methotrexate is commonly used as anticancer and anti-inflammatory agent to cure various types of cancerous and auto-immune disorders. An optimum dose of MXT is proven to inhibit the di-hydro-folate-reductase that obstruct the purine multiplication. The nanotechnology-based carriers have outranged in since decade and fabricated as multifunctional complexes to cater medicinal agents for biomedical and pharmaceutical applications. The present review aims on upbringing the understanding the various formulation development of MXT-loaded nanocarriers that have been reported with significance in the treatment of cancers. Also, in this paper, we have comprehensively listed various marketed MXT nanoformulation available in the market with a great safety, efficacy and been promising with great results in patients across the globe.