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Continuous release of gentamicin from gold nanocarriers

机译:从金纳米载体中连续释放庆大霉素

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Antibiotics are still the most effective agents used to fight bacterial infections. Antibiotics are quickly metabolised or excreted from the human body, thus they need to be frequently administered (a few times a day) and their half life is usually an important factor in the therapeutic choice. In order to render the administration less frequent, antibiotic release from a carrier can be employed. In this work we covalently bound gentamicin to gold nanoparticles capped with cysteine or glutathione as gold nanoparticles are biologically safe. The conjugates exhibited antimicrobial activity against both S. aureus and MRSA at concentrations as low as 0.1 mg NP per ml consistent with an antibiotic load of 1-2% w/w as determined through TGA. No antimicrobial activity was exhibited by the unconjugated nanoparticles. The release of gentamicin from the conjugates was monitor in buffer solutions at pH = 7 and the antibiotic concentration continued to increase over two days. This work demonstrates that gold nanoparticles can be employed as antibiotic carriers providing a continuous release of antibiotic over a few days. Glutathione appeared to be a better coupling agent than cysteine allowing a higher load of gentamicin resulting in lower inhibitory concentrations of the conjugates.
机译:抗生素仍然是抵抗细菌感染的最有效药物。抗生素会迅速从人体中代谢或排出体外,因此需要经常服用(一天几次),并且半衰期通常是治疗选择的重要因素。为了降低给药频率,可以采用从载体释放抗生素的方法。在这项工作中,我们将庆大霉素与半胱氨酸或谷胱甘肽加帽的金纳米粒子共价结合,因为金纳米粒子具有生物安全性。缀合物在低至0.1 mg NP / ml的浓度下对金黄色葡萄球菌和MRSA均表现出抗菌活性,这与通过TGA测定的1-2%w / w的抗生素载量一致。未结合的纳米颗粒没有表现出抗菌活性。在pH = 7的缓冲溶液中监测庆大霉素从结合物中的释放,并且抗生素浓度在两天内持续增加。这项工作表明金纳米颗粒可以用作抗生素载体,在几天内连续释放抗生素。谷胱甘肽似乎是比半胱氨酸更好的偶联剂,允许更高的庆大霉素负载量,从而降低了结合物的抑制浓度。

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