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万古霉素从可生物降解微球中的体内释放

In vivo release of vancomycin from biodegradable beads.

作者信息

Liu Shih-Jung, Wen-Neng Ueng Steve, Lin Song-Shu, Chan Err-Cheng

机构信息

Department of Mechanical Engineering, Chang Gung University, Tao-Yuan, Taiwan.

出版信息

J Biomed Mater Res. 2002;63(6):807-13. doi: 10.1002/jbm.10406.

Abstract

The current delivery system of antibiotics for the treatment of osteomyelitis uses polymethylmethacrylate (PMMA) beads as a local drug-release agent. The nonbiodegradable nature of the PMMA, however, necessitates a second operation to remove the beads. This article explores the alternative of using biodegradable polymers as antibiotic beads for a long-term drug release in vivo. To manufacture an antibiotic bead, lactide-glycolide copolymers were mixed with vancomycin. The mixture was compressed and sintered at 55 degrees C to form beads 8 mm in diameter. An in vivo animal model was proposed to characterize the elution rate of antibiotic over a 55-day period. Biodegradable beads released high concentrations of antibiotic (well above the breakpoint sensitivity concentration) in vivo for the period of time needed to treat bone infection; that is, 4-6 weeks. A bacterial inhibition test was also carried out to determine the relative activity of the released antibiotics. The diameter of the sample inhibition zone ranged from 8 to 18 mm, which is equivalent to 9.1 to 100% of relative activity. In addition, the antibiotic concentration of systemic blood was found to be very low. Antibiotic-impregnated biodegradable beads may have a potential role in the prevention and management of surgical infections.

摘要

目前用于治疗骨髓炎的抗生素递送系统使用聚甲基丙烯酸甲酯(PMMA)珠作为局部药物释放剂。然而,PMMA的不可生物降解性质需要进行二次手术来取出珠子。本文探讨了使用可生物降解聚合物作为抗生素珠在体内进行长期药物释放的替代方法。为了制造抗生素珠,将丙交酯-乙交酯共聚物与万古霉素混合。将混合物在55℃下压缩并烧结以形成直径为8mm的珠子。提出了一种体内动物模型来表征55天内抗生素的洗脱速率。可生物降解的珠子在治疗骨感染所需的时间段内,即4至6周内,在体内释放高浓度的抗生素(远高于断点敏感浓度)。还进行了细菌抑制试验以确定释放的抗生素的相对活性。样品抑制区的直径范围为8至18mm,相当于相对活性的9.1%至100%。此外,发现全身血液中的抗生素浓度非常低。抗生素浸渍的可生物降解珠子可能在手术感染的预防和管理中具有潜在作用。

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