Bone morphogenetic protein-2 binds as multilayers to a collagen delivery matrix: an equilibrium thermodynamic analysis

Biomacromolecules. 2006 Jan;7(1):131-8. doi: 10.1021/bm050461i.

Abstract

Recombinant human bone morphogenetic protein-2 (rhBMP-2) promotes bone growth but must be retained at the delivery site for optimal efficacy in vivo. rhBMP-2 release from a collagen-based matrix has shown favorable pharmacokinetics. The present study assessed binding affinity and binding saturation of rhBMP-2 to a collagen matrix as a function of solution and rhBMP-2 isoform variables. Results indicate that rhBMP-2 binds to the collagen matrix with affinities on the order of 10(3) to 10(4) M(-1). Maximum binding, nu, was primarily a function of pH for heterogeneous rhBMP-2 and the extended (T(266)/T(266)) isoform. However, binding saturation of the <Q(283)/<Q(283) isoform was unaffected by pH. Overall, binding saturation was higher than the calculated saturation of a rhBMP-2 monolayer, suggesting both hydrophobic and ionic interactions in a multilayer formation. The contributions of pH and ionic strength to the linkage free energy of interaction was on the order of 1.3 kcal mol(-1) and approximately 0.3 kcal mol(-1), respectively. This thermodynamic approach can serve to optimize interactions between therapeutic proteins and delivery systems.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Bone Morphogenetic Protein 2
  • Bone Morphogenetic Proteins / chemistry*
  • Bone Morphogenetic Proteins / metabolism*
  • Bone Morphogenetic Proteins / pharmacokinetics
  • Chromatography, High Pressure Liquid
  • Collagen / chemistry*
  • Collagen / metabolism*
  • Humans
  • Kinetics
  • Protein Binding
  • Protein Isoforms / chemistry
  • Protein Isoforms / metabolism
  • Thermodynamics
  • Transforming Growth Factor beta / chemistry*
  • Transforming Growth Factor beta / metabolism*
  • Transforming Growth Factor beta / pharmacokinetics

Substances

  • BMP2 protein, human
  • Bone Morphogenetic Protein 2
  • Bone Morphogenetic Proteins
  • Protein Isoforms
  • Transforming Growth Factor beta
  • Collagen