Nanoparticle-mediated therapy represents a groundbreaking approach in the treatment of brain tumours, offering enhanced targeting, delivery, and efficacy of therapeutic agents. Brain tumours, including gliomas and metastatic brain cancers, present significant therapeutic challenges due to the difficulty of achieving effective drug concentrations within the brain while minimizing damage to surrounding healthy tissues. Traditional treatments, such as surgery, radiation, and chemotherapy, often have limited success and substantial side effects. Nanoparticles offer several advantages in brain tumour therapy. Their ability to encapsulate chemotherapeutic agents, RNA interference molecules, or gene editing tools protects these agents from degradation, enhancing their stability and bioavailability. Surface modifications with ligands or antibodies enable nanoparticles to specifically target tumour cells, improving the precision of drug delivery and minimizing off-target effects. Additionally, nanoparticles can be engineered to cross the blood-brain barrier (BBB) through mechanisms like receptor-mediated transcytosis, ensuring the delivery of therapeutic agents directly to the tumour site. Furthermore, nanoparticles can be designed with stimuli-responsive properties, allowing for controlled and site-specific release of their payload in response to the tumour microenvironment, such as pH or enzymatic activity. This targeted approach not only maximizes therapeutic efficacy but also reduces systemic toxicity. Various types of nanoparticles, including liposomes, polymeric nanoparticles, dendrimers, and inorganic nanoparticles, have shown promising results in preclinical studies, demonstrating significant tumour regression and prolonged survival in animal models. This book chapter explores the innovative strategies, current progress, and future directions of nanoparticle-mediated therapy in the treatment of brain tumours, highlighting the potential to transform current therapeutic paradigms and improve patient outcomes. Continued research and clinical development are essential for overcoming existing challenges and fully realizing the benefits of this promising technology.