Article history: Received on: 17/01/2015 Revised on: 22/04/2015 Accepted on: 17/06/2015 Available online: 27/07/2015 The HIV/AIDS pandemic is an increasing global burden with devastating health-related and socioeconomic effects. The widespread use of antiretroviral therapy has dramatically improved life quality and expectancy of infected individuals. But currently available drug regimens and dosage forms are not good enough to eradicate HIV. Suboptimal adherence, toxicity, drug resistance and viral reservoirs make the lifelong treatment of HIV infection challenging. Along with some other organs, highly vascularized and secured with blood-brain barrier (BBB), brain acts as a great reservoir for the HIV virus. But all the available drug delivery techniques are not capable of bypassing the BBB and deliver anti-HIV drugs to the brain. In this review, all the brain delivery techniques available till date has been reviewed and recent noble ideas for delivering anti-HIV drugs to brain has been discussed.