脂质体粘菌素对耐药大肠杆菌的体外和体内抑菌活性研究

M. Fadel, H. Badr
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摘要

本研究旨在探讨脂质体包被粘菌素对耐药大肠杆菌的口服药代动力学、生物利用度、给药和药效的影响。O125敏感菌株(CS和LS)对黏菌素(C)和脂质体黏菌素(L)的最小抑制浓度(MIC)分别为1.56µg/ml和0.00156µg/ml,耐药菌株(CR和LR)对黏菌素的最小抑制浓度(MIC)分别为100µg/ml和0.025µg/ml。体外培养1hr后,脂质体粘菌素对敏感和耐药菌株O125的时间杀伤动力学在1 MIC下分别为100%和82.8%,在2 MIC下均为≥99.9%。通过单次口服100000 IU/kg b.wt的粘菌素和脂质体粘菌素,研究了健康鸡和病鸡的药代动力学/药理学特征。药动学参数;CS和CR的Cmax/MIC比值分别为3.5和0.06。脂质体粘菌素在LS和LR中分别为3.9x10 3和247.2。CS、CR、LS和LR的AUC/MIC分别为13.4、0.248、40.9 x10.3和2.6 x10.3;证明了脂质体粘菌素的高疗效,粘菌素活性不显著。脂质体粘菌素组的t1 /2 β和MRT均显著高于粘菌素组。相反,脂质体粘菌素组的清除率(CL/F)明显低于粘菌素组。脂质体粘菌素使生物利用度由5.2%提高到49.2%。连续5 d反复处理后,两菌株肝脏大肠杆菌计数均呈极显著下降,与阴性对照组基本相似;说明脂质体粘菌素对两种大肠杆菌均有显著的作用,尤其是对耐粘菌素菌株。本研究推荐脂质体粘菌素制剂对抗多重耐药大肠杆菌感染。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Antimicrobial activity of Liposomal colistin against resistant E. coli in vitro and in vivo
T his study was performed to investigate the liposome coated colistin for enhancing the oral pharmacokinetics, bioavailability, delivery and efficacy of the drug against resistant E. coli strain. Minimum inhibitory concentration (MIC) of colistin (C) and liposomal colistin (L) was 1.56 µg/ml and 0.00156 µg/ml for O125 sensitive colistin strain (CS and LS), while 100µg/ml and 0.025 µg/ml for O125 resistant strain (CR and LR). In vitro, time kill kinetics of liposomal colistin against sensitive and resistant O125 recorded 100% and 82.8% as a reduction% at 1 MIC, while ≥99.9% at 2 MIC for both strains after 1hr incubation time. The pharmacokinetic/ pharmacodynamics profiles were studied by single oral dose of colistin and liposomal colistin at 100000 IU/kg b.wt in healthy and diseased chicken. The pharmacokinetic parameters; Cmax/MIC ratio for CS and CR were 3.5 and 0.06. While, liposomal colistin recorded 3.9x10 3 and 247.2 for LS and LR, respectively. AUC/MIC ratios were 13.4, 0.248, 40.9x10 3 and 2.6x10 3 for CS, CR, LS and LR, respectively; proving the high efficacy of liposomal colistin with less significant activity of colistin. There was significant increment of t 1/2 Beta and MRT of liposomal colistin groups in comparison with colistin groups. Contraries, clearance Time (CL/F) was significantly decreased in liposomal colistin than colistin groups. Liposomal colistin en-hanced the bioavailability% from 5.2% to 49.2%. Liver E. coli count re-vealed highly significant decrease of LC for both strains nearly similar to negative control group after repeated treatment for 5 consecutive days; indicating the great effect by liposomal colistin on both E. coli strains especially for colistin resistant strain. This study recommends the liposomal colistin formulation against multidrug resistant E. coli infections.
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