Synthesis and characterization of surface‐modified PBLG nanoparticles for bone targeting: In vitro and in vivo evaluations

摘要: In this study, poly(γ-benzyl-l-glutamate) (PBLG) polypeptide derivatives were synthesized by ring-opening polymerization of amino acid N-carboxyanhydride using selected amine-terminated initiators. Alendronate, a targeting moiety that has strong affinity for bone, was conjugated to PBLG. Monomethoxy polyethylene glycol (PEG) used hydrophilic layer on the surface nanoparticles (NPs) avoid reticuloendothelial system uptake. NPs prepared nanoprecipitation technique not only PBLG or PBLG–PEG but also composite polymers with different ratios. Fluorescein isothiocyanate would be attached as labeling agent. The size and morphology evaluated dynamic laser light scattering transmission electron microscopy, found in useful range (less than 80 nm) bone-targeted drug delivery. addition, PEGylation supported isothermal titration calorimetry analysis. bone-targeting potential vitro calcium binding hydroxyapatite assays, vivo fluorescent imaging experiments rats. targeted showed bright femur tissue. These results demonstrated possibility optimized new accumulate bone successfully. © 2011 Wiley-Liss, Inc. American Pharmacists Association J Pharm Sci 100:4877–4887,