Stallmann Hein P, Faber Christopher, Slotema Eveline T, Lyaruu D M, Bronckers Antonius L J J, Amerongen Arie V Nieuw, Wuisman Paul I J M
Department of Orthopaedic Surgery/VU University Medical Center, PO Box 7057, Amsterdam, The Netherlands.
J Antimicrob Chemother. 2003 Nov;52(5):853-5. doi: 10.1093/jac/dkg443. Epub 2003 Sep 30.
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.
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).
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.
Different release profiles may be obtained by choosing the appropriate carrier, which supports the feasibility of biodegradable carriers releasing AMPs against resistant infections.
为了确定针对耐药性骨感染的可能的药物递送系统，我们测定了抗菌肽（AMP）人乳铁蛋白1-11（hLF1-11）从市售骨替代物中的释放情况。
我们将六种磷酸钙骨水泥和六种颗粒类型与5mg/g的hLF1-11混合，并测定其在体外从骨水泥（7天）和颗粒（3天）中的可用性和释放情况。使用质谱法和对耐甲氧西林金黄色葡萄球菌（MRSA）的杀伤试验，测定了在前24小时内释放的hLF1-11的完整性和抗菌活性。
大多数骨水泥表现出突释，随后是低水平的持续释放，而包衣颗粒在24小时内表现出高突释。释放后，该肽具有活性（12种材料中的9种）且完整。
通过选择合适的载体可以获得不同的释放曲线，这支持了可生物降解载体释放AMP以对抗耐药性感染的可行性。
