The treatment of brain tumour is a challenging task for the physicians and the scientists who are involved in the research of development of proper drug delivery systems. It is because of the presence of blood brain barrier (BBB) as well as P-gp efflux pump which produces restriction in the transportation of drug into brain. Hence it is envisaged to develop such delivery system which will not only help to deliver anticancer drug to brain but also target the brain tumour cells. Present invention relates to the drug delivery system consisted of surface modified (i.e., appended with transferrin) PLGA nanoparticles bearing ligand conjugated anticancer drug (i.e Paclitaxel: Hyaluronic acid Bioconjugate). The transferrin attached to the surface of PLGA nanoparticle is helping nanoparticles to cross the BBB by a receptor mediated endocytosis while paclitaxil-HA Bioconjugate directs the drug to brain tumour site as CD44 receptors are over expressed on brain tumour cells which are responsible receptors for HA uptake. The concluded that transferrin coupled PLGA nanoparticles bearing Paclitaxel-HA bioconjugate are the potential carrier for targeting the anticancer drug to the brain tumour.