Lenvatinib (LEN), a tyrosine kinase inhibitor, has emerged as a promising therapeutic agent for various solid tumors. Nevertheless, a number of constraints, including diminished bioavailability, incapacity to elicit localized inflammation, and inability to selectively accumulate at the tumor site, may impede the comprehensive exploitation of its versatile tyrosine kinase inhibitory capabilities. In order to achieve targeted delivery of LEN while also reducing its high dose used in conventional therapeutics, nanoformulation approaches can be adopted. The integration of LEN into various nanoformulations, such as nanoparticles, nanocrystals, high density lipoproteins (HDLs), liposomes, and micelles, is discussed, highlighting the advantages of these innovative approaches in a comparative manner; however, given that the current methods of nanoformulation synthesis employ toxic organic solvents and chemicals, there is an imperative need for exploring alternative, environmentally friendly approaches. The multifaceted effects of nanocarriers have rendered them profoundly applicable within the biomedical domain, serving as instrumental entities in various capacities such as vehicles for drug delivery and genetic material, diagnostic agents, facilitators of photothermal therapy, and radiotherapy. However, the scalability of these nanotechnological methodologies must be rigorously investigated and addressed to refine drug delivery mechanisms. This endeavor offers promising prospects for revolutionizing strategies in cancer therapeutics, thereby laying the foundation for future research in scale-up techniques in the pursuit of more effective and less toxic therapies for cancer.