The present invention relates to preparation and characterization of HAART combination 655 anti-retroviral drugs loaded lactoferrin nanoparticles for first line and second line therapy. The first line drug combination is Zidovudine (AZT), Efavirenz (EFV) and Lamivudine (LMV) and the second line drug combination is Tenofovir (TNF), Lamivudine (LMV) and Atazanavir (ATV) / Ritonavir (r). The formulated drugs are especially suitable to be administered orally. The nanoformulation enhances anti-HIV activity of drugs along with 660 significant decrease in drug-related toxicity and improvement in bioavailability and PK profile of the drugs.