BIODEGRADABLE CONTROLLED ANTIBIOTIC RELEASE DEVICES FOR OSTEOMYELITIS - OPTIMIZATION OF RELEASE PROPERTIES
BIODEGRADABLE CONTROLLED ANTIBIOTIC RELEASE DEVICES FOR OSTEOMYELITIS - OPTIMIZATION OF RELEASE PROPERTIES
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DOI：
10.1111/j.2042-7158.1994.tb03890.x
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发表时间：
1994-09-01
影响因子：
3.3
通讯作者：
GOOSEN, MFA
中科院分区：
文献类型：
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作者：
ZHANG, XC;WYSS, UP;GOOSEN, MFA
由可生物降解的聚（D， l -丙交酯）（PDLLA）和聚（D， l -丙交酯- co -epsilon-己内酯）制成控制抗生素释放膜、熔融挤出瓶和悬浮挤出/涂覆瓶。这些装置在骨髓炎的治疗中具有潜在的应用价值。在药量从16%到50%不等的情况下，检测了该装置的体外释放特性。硫酸庆大霉素薄膜和熔融挤压庆大霉素/PDLLA圆柱体表现出大的初始爆裂和不完全释放。由聚（D， l -乳酸- co -epsilon-己内酯）、低摩尔重量聚（D， l -乳酸）以及D， l -乳酸低聚物和高摩尔重量聚（D， l -乳酸）的混合物制成的薄膜和熔融挤压圆柱体在整个释放期间并没有保持完整。虽然这是不希望的，但这些材料确实具有不需要超过110摄氏度的加工温度的优点。抗生素从高摩尔重量的PDLLA涂层庆大霉素/PDLLA圆柱体中释放，装载量为40%和50%，非常迅速。抗生素只能从圆柱体的开口端扩散出去。包被硫酸庆大霉素药量为20%和30%的圆柱体在小的初始爆发和逐渐持续释放方面表现出最有希望的特性。通过将涂层圆筒切割成不同长度，可调节其释放速度和持续时间；将90%的包埋庆大霉素从长度为0.2、0.4、0.7和1 cm的30%负载的pdla包被瓶中释放到水中所需的时间分别为1000、1700、2300和2800 h。这提供了一种方便的方法来调整释放，以满足不同患者的特定抗生素需求。头孢唑啉和青霉素由于在水中水解不稳定，不适于300h以上的缓释。
Controlled antibiotic release films, melt-extruded cylinders, and suspension-extruded/coated cylinders were manufactured from biodegradable poly(D,L-lactide) (PDLLA) and poly(D,L-lactide-CO-epsilon-caprolactone). These devices have potential application in the treatment of osteomyelitis. The in-vitro release properties of the devices were examined with drug loadings varying from 16 to 50%. Gentamicin sulphate films and melt-extruded gentamicin/PDLLA cylinders demonstrated a large initial burst and incomplete release. The films and melt-extruded cylinders made from poly(D,L-lactide-CO-epsilon-caprolactone), low mol. wt poly(D,L-lactide), and a mixture of D,L-lactic acid oligomer and high mol. wt poly(D,L-lactide), did not remain intact during the entire release period. While this is undesirable, these materials do have the advantage of not requiring a processing temperature of greater than 110 degrees C. Antibiotic release from high mol. wt PDLLA-coated gentamicin/PDLLA cylinders, with 40 and 50% loading, was very rapid. The antibiotic could only diffuse out through the open ends of the cylinder. Coated gentamicin sulphate cylinders with 20 and 30% drug loading gave the most promising properties in terms of a small initial burst, and a gradual and sustained release. The release rate and duration from the coated cylinders could be adjusted by cutting the cylinder into different lengths; the time required for 90% of the entrapped gentamicin to be released into water from 30% loaded PDLLA-coated cylinders 0.2, 0.4, 0.7 and 1 cm in length was 1000, 1700, 2300, and 2800 h, respectively. This offers a convenient method to adjust the release to meet the specific antibiotic requirement of different patients. Cephazolin and benzylpenicillin were found to be unsuitable for sustained release longer than 300 h due to the hydrolytic instability of the drugs in water.