Background: The invention of an efficacious drug delivery system for the treatment of HIV/AIDS still remains a worldwide problem and presently, an ideal remedy for HIV/AIDS is not available. One of the greatest achievements in transforming HIV infection into a chronically managed disease is anti-retroviral therapy (ART) including Highly Active Antiretroviral Therapy (HAART) which has increased the life span and improved the quality of life of the HIV/AIDS patient. But, the lack of widespread preventive measures and the inability of anti-retroviral (ARV) drugs to eliminate HIV from infected cells still remain a challenge. Also, the current ARVs are unable to reach the HIV viral load present in the brain which is one of the important sanctuary sites for the HIV virus.Objective: Thus, now is the time to explore nanotechnology and its potential in the treatment and prevention of HIV/AIDS. Particularly, nanocarriers, which are lipidic in nature, have proven to be beneficial in the case of ARV drugs. Conclusion: Lipid based ARV formulations protect the compounds from degrading and enhance the potency as well as reduce the toxicity of the drug. This review focusses on the emergence of polymeric and lipid based nanocarriers with major emphasis on lipid based drug delivery system.