Piozzi A, Francolini I, Occhiaperti L, Di Rosa R, Ruggeri V, Donelli G
Department of Chemistry, University of Rome La Sapienza, Piazzale Aldo Moro 5, 00185 Rome, Italy.
J Chemother. 2004 Oct;16(5):446-52. doi: 10.1179/joc.2004.16.5.446.
Acidic or basic polyurethanes were loaded with antibiotics to develop materials to prevent medical device-related infections. A correlation between polymer-antibiotic interactions and amount of drug absorbed by polymers and released over time was found. Since the employed antibiotics, i.e. amoxicillin, cefamandole nafate, rifampin and vancomycin, possessed at least an acidic group in their structural formula, the introduction of basic tertiary amines in the polyurethane side-chain resulted in an increased polymer ability to adsorb antibiotics. However, a stronger ionic interaction between this polymer and the antibiotics caused a release of lower amount of drug over time. Antibiotics released from polymers inhibited Staphylococcus epidermidis growth on agar. Antibiotic-loaded polyurethanes kept in water for increasing times were still able to show inhibition zones of bacterial growth. The antibacterial activity lasted up to 3 hours for amoxicillin, 24 hours for vancomycin, 8 days for cefamandole nafate and 8 months for rifampin.
酸性或碱性聚氨酯负载抗生素以开发预防与医疗器械相关感染的材料。发现聚合物与抗生素之间的相互作用与聚合物吸收并随时间释放的药物量之间存在相关性。由于所使用的抗生素，即阿莫西林、头孢孟多酯钠、利福平和万古霉素，在其结构式中至少含有一个酸性基团，因此在聚氨酯侧链中引入碱性叔胺会提高聚合物吸附抗生素的能力。然而，这种聚合物与抗生素之间更强的离子相互作用导致随时间释放的药物量减少。从聚合物中释放的抗生素抑制了表皮葡萄球菌在琼脂上的生长。在水中放置不同时间的负载抗生素的聚氨酯仍然能够显示出细菌生长抑制圈。阿莫西林的抗菌活性持续长达3小时，万古霉素为24小时，头孢孟多酯钠为8天，利福平为8个月。
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