Surface biofunctionalization of PLA nanoparticles through amphiphilic polysaccharide coating and ligand coupling: Evaluation of biofunctionalization and drug releasing behavior

The purpose of present study was to conceive small-sized nanoparticles which can be easily functionalized with ligands and meanwhile minimized drug leakage. For this purpose, cholesterol-modified dextran dialdehyde was synthesized and used to prepare indomethacin loaded PLA nanoparticles containing aldehyde groups on surface. Transferrin (TF) was coupled to their surface by taking advantage of the Schiff's base reaction and the effect of ligand coupling on drug leakage was evaluated. The results show that the coupling process reached equilibrium within 5 min and less than 20% drug was leaked after NaBH4 reduction. TF coupled nanoparticles was fluorescence labeled with FITC, and cell uptake experiment was performed in vitro. The result demonstrated the bioactivity of TF after binding on nanoparticles and the ability of the nanoparticles targeting to tumor cell mediated by ligand-receptor interaction. (c) 2006 Elsevier Ltd. All rights reserved.