Most of the time HIV virus escape immunological burden exerted by antiretroviral drugs and develops resistance against therapy. For complete eradication of virus from body one has to use long term chemotherapies, which results in drug toxicity, drug resistance and eventually poor patient compliance. Nevirapine (NNRTI, non nucleoside reverse transcriptase inhibitor) nanosuspensions were developed and surface modified with serum albumin, polysaccharide and polyethylene glycol to enhance its targeting potential. The biodistribution studies revealed improved antiretroviral drug accumulation in various organs of rat for nanosuspensions as compared to the plain drug solution when administered intravenously. Nanosuspension after surface modification showed further enhancement in accumulation. Higher MRT values of surface coated nanosuspension in brain, liver and spleen as compared to pure drug solution ensured enhanced bioavailability and prolonged residence of the drug at the target site.