Liu Shih-Jung, Tsai Ying-E, Wen-Neng Ueng Steve, Chan Err-Cheng
Department of Mechanical Engineering, Biomaterials Lab, Chang Gung University, 259, Wen-Hwa 1st Road, Kwei-San, Tao-Yuan 333, Taiwan.
Biomaterials. 2005 Aug;26(22):4662-9. doi: 10.1016/j.biomaterials.2004.11.053. Epub 2005 Jan 13.
This report was to develop a novel solvent-free method for the manufacture of biodegradable capsules for a long-term drug delivery. To manufacture an antibiotic capsule, polylactide-polyglycolide copolymers were pre-mixed with vancomycin. The mixture was then injection compression molded to form a cylinder with a cover of 8mm in diameter. After the addition of gentamicin sulfate into the core, an ultrasonic welder was used to seal the capsule. An elution method and an high-performance liquid chromatography assay were employed to characterize the in vitro release rates of the antibiotics over a 30-day period. It was found that biodegradable capsules released high concentration of vancomycin and gentamicin (well above the minimum inhibition concentration) in vitro for the period of time needed to treat bone infection; i.e., 2-4 weeks. A bacterial inhibition test was carried out to determine the relative activity of the released antibiotics. The diameter of the sample inhibition zone ranged from 3 to 18 mm, which is equivalent to 16.7-100% of relative activity. By adopting this novel technique, we will be able to manufacture biodegradable capsules of various medicines for long-term drug delivery.
本报告旨在开发一种新型无溶剂方法，用于制造用于长期药物递送的可生物降解胶囊。为制造抗生素胶囊，将聚丙交酯-聚乙交酯共聚物与万古霉素预混合。然后将混合物注射压缩成型，形成一个直径为8毫米、带有封盖的圆柱体。在向芯部加入硫酸庆大霉素后，使用超声波焊接机密封胶囊。采用洗脱法和高效液相色谱分析法来表征抗生素在30天内的体外释放速率。结果发现，可生物降解胶囊在治疗骨感染所需的时间段（即2至4周）内，在体外释放出高浓度的万古霉素和庆大霉素（远高于最低抑菌浓度）。进行了细菌抑制试验以确定释放抗生素的相对活性。样品抑菌圈直径范围为3至18毫米，相当于相对活性的16.7%至100%。通过采用这种新技术，我们将能够制造用于各种药物长期药物递送的可生物降解胶囊。
