Continuous-release or burst-release of the antimicrobial peptide human lactoferrin 1-11 (hLF1-11) from calcium phosphate bone substitutes

J Antimicrob Chemother. 2003 Nov;52(5):853-5. doi: 10.1093/jac/dkg443. Epub 2003 Sep 30.

Abstract

Objectives: In order to identify possible drug delivery systems against resistant bone infection, we determined the release of the antimicrobial peptide (AMP) human lactoferrin 1-11 (hLF1-11) from commercially available bone substitutes.

Methods: We combined six calcium phosphate cements and six granule-types with 5 mg/g hLF1-11 and measured its availability and release in vitro from cements (7 days) and granules (3 days). The integrity and antimicrobial activity of the hLF1-11 that was released during the first 24 h were measured, using mass spectrometry, and a killing assay on methicillin-resistant Staphylococcus aureus (MRSA).

Results: Most of the cements showed burst release followed by low-level continuous release, whereas the coated granules showed high burst release for 24 h. After release the peptide was active (in nine of 12 materials) and intact.

Conclusions: Different release profiles may be obtained by choosing the appropriate carrier, which supports the feasibility of biodegradable carriers releasing AMPs against resistant infections.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biodegradation, Environmental
  • Bone Substitutes / chemistry*
  • Calcium Phosphates / chemistry*
  • Drug Delivery Systems / methods*
  • Humans
  • Lactoferrin
  • Mass Spectrometry
  • Methicillin Resistance
  • Peptide Fragments / chemistry*
  • Peptide Fragments / pharmacology*
  • Staphylococcus aureus / drug effects*

Substances

  • Bone Substitutes
  • Calcium Phosphates
  • Peptide Fragments
  • alpha-tricalcium phosphate
  • lactoferrin (1-11), human
  • tetracalcium phosphate
  • calcium phosphate, monobasic, anhydrous
  • calcium phosphate
  • Lactoferrin
  • calcium phosphate, dibasic, anhydrous