Brain tumors pose a substantial challenge due to their location within the brain and the existence of the Blood-Brain Barrier (BBB), which confines the access to many therapeutic agents. This article provides an overview of brain tumors, their cataloguing, causes, and symptoms, highlighting the life-threatening nature of these tumors. The main focus of this article is the novel approach of active targeting in nanoformulation for brain tumors by means of lactoferrin (Lf) as an active targeting ligand. The BBB's impermeability hampers the delivery of therapeutic agents to brain tumors, making it essential to find efficient drug delivery systems. Nanoparticles fabricated from various polymers such as synthetic and biopolymers have shown promise in this regard due to their diverse nature and biocompatibility. This includes a method using lactoferrin, a protein with iron-binding properties, as an active targeting ligand to improve brain tumor drug delivery. with highlighting the increasing research interest in using lactoferrin-based nanoparticles in cancer therapy, and the potential application of lactoferrin as a drug nanocarrier in the field of nanomedicine.