Department of Pharmaceutics and Nanotechnology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Students' Research Committee, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Drug Dev Ind Pharm. 2020 Aug;46(8):1209-1218. doi: 10.1080/03639045.2020.1788058. Epub 2020 Jul 8.
To evaluate the effect of ciprofloxacin concentration and cement geometry on release, mechanical, and antibacterial properties of PMMA bone cement. Cements are used in different geometries and drug concentrations. These can affect cement strength, drug release behavior, and its antibacterial activity.
Antibiotic-loaded bone cement (ALBC) containing 2.5, 5.0, and 10.0 wt% ciprofloxacin were prepared as slab, rectangular prism and short cylinder. Drug release and compression strength of the cements were investigated for 28 days at 37 °C. The ALBC efficacies against prevalent bone infection bacteria, , , and , were investigated. Drug determination was by HPLC.
A two-stage behavior of fast release through dissolution/diffusion (stage A; <96 h) and 2-5 times slower Fickian diffusion (stage B; 96-672 h) was observed. Significant differences for release rate were observed among different geometries in the order of cylinder > prism > slab, in correlation with systems' thickness, indicating lower drug depletion in thicker systems. Release rates were proportional to concentration for 2.5 and 5% systems. At 10.0% loading, however, apparently interconnected channels and higher porosity reduced the diffusional resistance and provided higher release rates than what expected from concentration increment. Growth of Gram-negative bacteria and was inhibited at the lowest dose of drug over 1 and 48 h, respectively. ALBCs with 5.0 and 10.0% ciprofloxacin showed decrease of compression strength to below ISO standard.
Different properties of acrylic cements are affected by geometry and drug concentration and should be considered for optimized drug therapy.
评估环丙沙星浓度和水泥几何形状对 PMMA 骨水泥释放、力学和抗菌性能的影响。水泥以不同的几何形状和药物浓度使用。这些因素会影响水泥强度、药物释放行为及其抗菌活性。
制备含 2.5%、5.0%和 10.0%wt%环丙沙星的载药骨水泥（ALBC），形状分别为平板、长方体和短圆柱体。在 37°C 下研究水泥 28 天内的药物释放和压缩强度。研究了 ALBC 对常见骨感染细菌 、 、 、和 的疗效。药物测定采用 HPLC 法。
观察到快速释放的两阶段行为，通过溶解/扩散（阶段 A；<96h）和 2-5 倍较慢的菲克扩散（阶段 B；96-672h）。不同几何形状的释放速率存在显著差异，顺序为圆柱体>长方体>平板，与系统厚度相关，表明较厚系统中药物耗竭较少。对于 2.5%和 5%的系统，释放速率与浓度成正比。然而，在 10.0%的载药量下，显然相互连接的通道和更高的孔隙率降低了扩散阻力，并提供了比预期更高的释放速率。在最低药物剂量下，革兰氏阴性菌和 生长在 1 和 48 小时内分别被抑制。含 5.0%和 10.0%环丙沙星的 ALBC 压缩强度降至低于 ISO 标准。
不同的丙烯酸水泥性能受几何形状和药物浓度的影响，应考虑优化药物治疗。
