Treatment of brain tumour is a major challenge. This is mainly because of the limited bioavailability of chemotherapeutics in the brain. The major hurdle for brain availability of anticancer agents is the blood brain barrier (BBB). BBB is supposed to protect the brain and maintain homeostasis. It allows vital nutrient for normal brain function and effluxes out foreign toxic substance. Advance in knowledge of bidirectional movement across BBB has allowed development of strategies to enhance brain availability of chemotherapeutics for management of brain tumour. In this review we have focussed on various approaches adopted for enhancing delivery of anticancer agents. We have given a critical analysis of the approaches for further research
Keywords: Brain, chemotherapy, delivery, tumour.