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首页> 外文期刊>Antimicrobial agents and chemotherapy. >Ciprofloxacin in Polyethylene Glycol-Coated Liposomes: Efficacy in Rat Models of Acute or Chronic Pseudomonas aeruginosa Infection.
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Ciprofloxacin in Polyethylene Glycol-Coated Liposomes: Efficacy in Rat Models of Acute or Chronic Pseudomonas aeruginosa Infection.

机译：环丙沙星在聚乙二醇包衣脂质体中的作用：在急性或慢性铜绿假单胞菌感染大鼠模型中的功效。

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In a previous study in experimental Klebsiella pneumoniae pneumonia, the therapeutic potential of ciprofloxacin was significantly improved by encapsulation in polyethylene glycol-coated ("pegylated") long-circulating (STEALTH) liposomes. Pegylated liposomal ciprofloxacin in high doses was nontoxic and resulted in relatively high and sustained ciprofloxacin concentrations in blood and tissues, and hence an increase in the area under the plasma concentration-time curve (AUC). These data correspond to data from animal and clinical studies showing that for fluoroquinolones the AUC/MIC ratio is associated with favorable outcome in serious infections. Clinical failures and the development of resistance are observed for marginally susceptible organisms like Pseudomonas aeruginosa and for which sufficient AUC/MIC ratios cannot be achieved. In the present study the therapeutic efficacy of pegylated liposomal ciprofloxacin was investigated in two rat models of Pseudomonas aeruginosa pneumonia. In the acute model pneumonia developed progressively, resulting in a rapid onset of septicemia and a high mortality rate. Ciprofloxacin twice daily for 7 days was not effective at doses at or below the maximum tolerated dose (MTD). However, pegylated liposomal ciprofloxacin either at high dosage or given at low dosage in combination with free ciprofloxacin on the first day of treatment was fully effective (100% survival). Obviously, prolonged concentrations of ciprofloxacin in blood prevented death of the animals due to early-stage septicemia in this acute infection. However, bacterial eradication from the left lung was not effected. In the chronic model, pneumonia was characterized by bacterial persistence in the lung without bacteremia, and no signs of morbidity or mortality were observed. Ciprofloxacin administered for 7 days at the MTD twice daily resulted in killing of more than 99% of bacteria in the lung; this result can also be achieved with pegylated liposomal ciprofloxacin given once daily. Complete bacterial eradication is never observed.
机译：在先前的实验性肺炎克雷伯菌肺炎研究中，环丙沙星的治疗潜力通过封装在聚乙二醇包衣的（“聚乙二醇化的”）长循环（STEALTH）脂质体中得到了显着改善。高剂量的聚乙二醇化脂质体环丙沙星无毒，可导致血液和组织中环丙沙星的浓度相对较高和持续水平，因此血浆浓度-时间曲线（AUC）下的面积增加。这些数据与来自动物和临床研究的数据相对应，这些数据表明，对于氟喹诺酮类药物，AUC / MIC比与严重感染的良好预后相关。对于像铜绿假单胞菌这样的边缘易受感染的生物，观察到临床失败和耐药性的发展，并且无法实现足够的AUC / MIC比。在本研究中，在两种铜绿假单胞菌肺炎大鼠模型中研究了聚乙二醇化脂质体环丙沙星的治疗效果。在急性模型中，肺炎逐渐发展，导致败血症的快速发作和高死亡率。每天两次连续7天的环丙沙星在最大耐受剂量（MTD）或以下时无效。但是，在治疗的第一天，高剂量或低剂量的聚乙二醇化脂质体环丙沙星与游离环丙沙星联合使用是完全有效的（100％存活率）。显然，长时间的血液中环丙沙星浓度可防止这种急性感染中由于早期败血病而导致动物死亡。但是，未实现从左肺根除细菌。在慢性模型中，肺炎的特征是肺中细菌持续存在而无菌血症，并且未观察到发病或死亡的迹象。每天两次在MTD上施用环丙沙星7天，导致肺中99％以上的细菌被杀死;每天一次给予聚乙二醇化脂质体环丙沙星也可以达到该结果。从未观察到完全根除细菌。

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