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Mol Pharm. 2012 Aug 6;9(8):2228-36. doi: 10.1021/mp3000748. Epub 2012 Jul 12.

Synthesis and evaluation of clickable block copolymers for targeted nanoparticle drug delivery.

Author information

1
Departments of †Chemical and Biological Engineering and ‡Molecular Biology, Princeton University , Princeton, New Jersey 08540, United States.

Abstract

Polymeric nanoparticles with multifunctional capabilities, including surface functionalization, hold great promise to address challenges in targeted drug delivery. Here, we describe a concise, robust synthesis of a heterofunctional polyethylene glycol (PEG), HO-PEG-azide. This macromer was used to synthesize polylactide (PLA)-PEG-azide, a functional diblock copolymer. Rapid precipitation of this copolymer with a hydrophobic cargo resulted in the generation of monodisperse nanoparticles with azides in the surface corona. To demonstrate conjugation to these nanoparticles, a regioselectively modified alkyne-folate was employed as a model small molecule ligand, and the artificial protein A1 with an alkyne moiety introduced by unnatural amino acid substitution was selected as a model macromolecular ligand. Using the copper-catalyzed azide-alkyne ligation reaction, both ligands exhibited good conjugation efficiency even when low concentrations of ligands were used.

PMID:
22734614
DOI:
10.1021/mp3000748
[Indexed for MEDLINE]

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