The incorporation of bioactive compounds in stealth nanoparticles or nanoemulsions enhances their half-life in systemic circulation and can overcome the problems associated with the free drug. Bovine serum albumin (BSA)–drug conjugates were produced with either methotrexate (MTX), a potent anticancer agent, or vancomycin (VCM), a potent antibiotic. Those conjugates were used to produce functionalized BSA nanoemulsions in a formulation composed of an aqueous phase and an organic phase. BSA–folic acid (FA) conjugates were also produced allowing specific folate receptor (FR) mediated targeting of cancer cells (KB cell line). All conjugates had similar effects either in solution or in the form of nanoemulsions: BSA–MTX as an anti-proliferative over the Caco-2 cell line and BSA–VCM with a lower minimum inhibitory concentration (MIC) compared to VCM solution on the Staphylococcus aureus strain Newman. The production of nanoemulsions using BSA–drug conjugates for obtaining vectors loaded with stabilized drugs offers a good, flexible template for a wide range of medical applications.