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Modern nanotechnology is an emerging field offering a dynamic tool for research in therapeutics. PLGA (Poly (lactide-coglycolide))
based nanoparticles offer an attractive option as in vivo drug delivery vehicle due to their biocompatibility,
efficient cellular uptake, rapid lysosomal escape and sustained drug release. PLGA nanoparticles can be employed for targeted
delivery of therapeutics by use of various surface ligands. Various studies have reported DV1 peptide ligand (derived from
vMIPII) to possess a high binding affinity for chemokine receptor CXCR4 and significant antiviral activity in inhibiting the
replication of CXCR4-dependent HIV-1 strains. Therefore, we aimed to target CXCR4 using Avidin-PLGA nanoparticles tagged
with biotinylated DV1 peptide ligand. Avidin-PLGA nanoparticles were prepared by double emulsion solvent evaporation
technique and size characterization done by Transmission Electron Microscope (particle diameter 50-200 nm). Surface
functionality of nanoparticles for avidin groups was ascertained by tagging them with Biotin-FITC conjugate and subsequently
treating U87MG cells with Biotin-FITC tagged NP and untagged NP followed by nanoparticle uptake analysis by confocal
microscope. For specific targeting of CXCR4 receptors, targeted nanoparticles (Peptide-Avidin PLGA NP) were prepared by
tagging biotinylated DV1 peptide onto the surface of avidin PLGA nanoparticles. Untagged nanoparticles were used as control
nanoparticles (Avidin PLGA NP). A significantly enhanced uptake of targeted nanoparticles in U87MG cells as compared to
Neuro-2a cells as analyzed by confocal microscopy confirm specificity of targeted nanoparticles for CXCR4 receptors. Our
results suggest that PLGA NP tagged with DV1 peptide can be used for targeted delivery which can have clinical application.