Cancer is a group of diseases characterised by uncontrollable, abnormal cell growth. Research scientists have had a difficult time dealing with cancerous brain tumours. Furthermore, the lack of early-stage symptoms delays its diagnosis, resulting in a worsening of the condition. Surgical, radiation, and chemotherapy treatments still have a number of drawbacks. It is difficult for most anticancer drugs to cross the blood–brain barrier, because of their low solubility and limited therapeutic window. Solid tumours can be targeted with nanoparticles that take advantage of the enhanced permeability and retention effect. Using surface membrane proteins that are over expressed in cancer cells as targets for active targeting, which involves altering the nanoparticles' surfaces, it is possible to reduce uptake in healthy tissue while increasing accumulation in tumours. Antibodies, their fragments, aptamers, oligopeptides, or small molecules are commonly used as target molecules. Several FDA-approved nanomedicines are currently available, but none of them has been approved for the treatment of brain tumours. The surface modified nanoparticles will lead to enhanced delivery of the drug to the brain by prevention of the clearance by reticuloendothelial system and probable inhibition of the efflux mechanism of brain and ultimately enhance drug concentration towards target site. This targeted drug delivery will lead to reduction in dose and also will reduce drug related toxicity towards normal cells.