unassigned: Chemokine receptor CXCR4 is frequently present in cells of various cancers. Hence, targeted therapy using CXCR4 ligands, such as DV1 peptide, on drug-loaded nanoparticles, has the potential to enhance the efficiency of cancer treatment. unassigned: The present study created a CXCR4-targeting drug delivery system using avidin-poly (lactic-co-glycolic acid) (PLGA) nanoparticle surface tagged with biotinylated DV1 peptide ligand. unassigned: A double-emulsion solvent evaporation technique was employed to prepare avidin-PLGA nanoparticles and characterized by transmission electron microscopy (TEM) and dynamic light scattering. Uptake was studied by confocal microscopy after incorporating fluorescein isothiocyanate (FITC)-labeled albumin inside the nanoparticles during their synthesis. Peptide-biotin-avidin-PLGA nanoparticles were tested on CXCR4-expressing U87MG cells. Photomicroscopy was done by a Nikon A1 Confocal Microscope, and pictures were analyzed by Nikon NIS-Elements BR software. unassigned: Experimental results confirmed the specificity of DV1 peptide-tagged avidin-PLGA nanoparticles for cells expressing CXCR4 receptors. The avidin-PLGA nanoparticles were successfully synthesized and the same was confirmed by tagging them with FITC-labeled biotin. unassigned: Avidin-PLGA nanoparticle surface tagged with biotinylated DV1 peptide ligand has potential clinical application in the treatment of various cancers as targeted therapy for CXCR4-expressing cancer cells.