Brain cancer is most fatal among various types of cancer. Here, solid-lipid nanoparticles, which are formed by tiny pores, are successfully synthesised. Anti-cancer drugs are encapsulated in each pore and the surface of the particles are modified with transferrin and RGD tripeptide. The particles are monodisperse in water and biocompatible/biodegradable. It has been proved by in vivo experiments that the drug encapsulated nanoparticles modified with transferrin and RGD penetrate the blood-brain barrier and reach brain tumours, as a result of which the target tumours are completely cured without showing any side effects. The optimal ratio of RGD to transferrin is obtained. The present methodology can be applied to the treatment of different types of cancer by changing the surface modification and drugs. Magnetic nanoparticles and quantum dots can be encapsulated in the present particles so that the particles can also be used for nano bio-imaging. The particles can be precisely manipulated by applying gradient dc magnetic fields, whereas they can be heated by applying high-frequency ac magnetic fields so that the drug release speed can be controlled and they can also be used for hyperthermia therapy.