The development of a suitable delivery system and the targeting of intracellular organelles are both essential for the success of drug and gene therapies. The conception of fluorescent ligands, displaying targeting specificity together with low toxicity, is an emerging and reliable tool to develop innovative delivery systems. Biocompatible BSA or pDNA/ligand nanoparticles were synthesized by a coprecipitation method and were shown to display adequate sizes and morphology for delivery purposes, and positive surface charges. Additionally, these fluorescent vectors can target specific intracellular organelles. In vitro transfection mediated by BSA or pDNA based carriers can result in the accumulation of BSA in the cytosol, lysosomes, and mitochondria or the expression of the plasmid-encoded protein, respectively. Moreover, the therapeutic effect of pDNA/ligand vectors in cancer gene therapy instigates further research aiming clinical translation.