Biofunctional polymer nanoparticles for intra-articular targeting and retention in cartilage

Nat Mater. 2008 Mar;7(3):248-54. doi: 10.1038/nmat2116. Epub 2008 Feb 3.

Abstract

The extracellular matrix of dense, avascular tissues presents a barrier to entry for polymer-based therapeutics, such as drugs encapsulated within polymeric particles. Here, we present an approach by which polymer nanoparticles, sufficiently small to enter the matrix of the targeted tissue, here articular cartilage, are further modified with a biomolecular ligand for matrix binding. This combination of ultrasmall size and biomolecular binding converts the matrix from a barrier into a reservoir, resisting rapid release of the nanoparticles and clearance from the tissue site. Phage display of a peptide library was used to discover appropriate targeting ligands by biopanning on denuded cartilage. The ligand WYRGRL was selected in 94 of 96 clones sequenced after five rounds of biopanning and was demonstrated to bind to collagen II alpha1. Peptide-functionalized nanoparticles targeted articular cartilage up to 72-fold more than nanoparticles displaying a scrambled peptide sequence following intra-articular injection in the mouse.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / therapeutic use
  • Biocompatible Materials / chemistry*
  • Cartilage / chemistry*
  • Cattle
  • Collagen Type II / chemistry
  • Collagen Type II / metabolism
  • Drug Delivery Systems
  • Injections, Intra-Articular
  • Joint Diseases / drug therapy*
  • Mice
  • Nanoparticles / chemistry*
  • Peptide Library
  • Peptides / chemistry
  • Polymers / chemistry*
  • Protein Binding

Substances

  • Anti-Inflammatory Agents
  • Biocompatible Materials
  • Collagen Type II
  • Peptide Library
  • Peptides
  • Polymers