Rasyid Hermawan N, van der Mei Henny C, Frijlink Henderik W, Soegijoko Soegijardjo, van Horn Jim R, Busscher Henk J, Neut Daniëlle
Department of Biomedical Engineering, University Medical Center Groningen and the University of Groningen, the Netherlands.
Acta Orthop. 2009 Oct;80(5):508-13. doi: 10.3109/17453670903389782.
Commercial gentamicin-loaded bone cement beads (Septopal) constitute an effective delivery system for local antibiotic therapy. These beads are not available in all parts of the world, and are too expensive for frequent use in others. Thus, orthopedic surgeons worldwide make antibiotic-loaded beads themselves. However, these beads are usually not as effective as the commercial beads because of inadequate release kinetics. Our purpose was to develop a simple, cheap, and effective formulation to prepare gentamicin-loaded beads with release properties and antibacterial efficacy similar to the commercially ones.
Acrylic beads were prepared with variable monomer content: 100% (500 microL/g polymer), 75%, and 50% to increase gentamicin release through creation of a less dense polymer matrix. Using the optimal monomer content, different gel-forming polymeric fillers were added to enhance the permeation of fluids into the beads. Polyvinylpyrrolidone (PVP) 17 was selected as a suitable filler; its concentration was varied and the antibiotic release and antibacterial efficacy of these beads were compared with the corresponding properties of the commercial ones.
Gentamicin release rate and the extent of release from beads prepared with 50% monomer increased when the PVP17 content was increased. Beads with 15 w/w% PVP17 released 87% of their antibiotic content. This is substantially more than the gentamicin release from Septopal beads (59%). Acrylic beads with 15 w/w% PVP17 reduced bacterial growth by up to 93%, which is similar to the antibacterial properties of the commercial ones.
A simple, cheap, and effective formulation and preparation process has been described for hand-made gentamicin-releasing acrylic beads, with better release kinetics and with antibacterial efficacy similar to that of the commercial ones.
商业化的载庆大霉素骨水泥珠（Septopal）构成了局部抗生素治疗的有效给药系统。这些珠子并非在世界所有地区都有供应，而在其他一些地区，其价格过高，无法频繁使用。因此，世界各地的骨科医生会自行制作载抗生素珠子。然而，由于释放动力学不充分，这些珠子通常不如商业化珠子有效。我们的目的是开发一种简单、廉价且有效的配方，以制备具有与商业化珠子相似的释放特性和抗菌效果的载庆大霉素珠子。
制备了具有不同单体含量的丙烯酸珠：100%（500微升/克聚合物）、75%和50%，通过创建密度较小的聚合物基质来增加庆大霉素的释放。使用最佳单体含量，添加不同的凝胶形成聚合物填料以增强流体渗入珠子的能力。选择聚乙烯吡咯烷酮（PVP）17作为合适的填料；改变其浓度，并将这些珠子的抗生素释放和抗菌效果与商业化珠子的相应特性进行比较。
当PVP17含量增加时，用50%单体制备的珠子的庆大霉素释放速率和释放程度增加。含15 w/w% PVP17的珠子释放了其87%的抗生素含量。这大大超过了Septopal珠子的庆大霉素释放量（59%）。含15 w/w% PVP17的丙烯酸珠使细菌生长减少高达93%，这与商业化珠子的抗菌特性相似。
已描述了一种用于手工制作载庆大霉素丙烯酸珠的简单、廉价且有效的配方和制备工艺，其具有更好的释放动力学，抗菌效果与商业化珠子相似。
