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Effect of liposome-entrapped ampicillin on survival of Listeria monocytogenes in murine peritoneal macrophages.

机译:脂质体包裹的氨苄青霉素对鼠腹膜巨噬细胞单核细胞增生李斯特菌存活的影响。

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摘要

The effect of liposomal encapsulation of ampicillin on the antibacterial activity against intracellular Listeria monocytogenes was studied by comparing survival of L. monocytogenes within peritoneal mouse macrophages in the presence of free ampicillin alone or in combination with liposome-entrapped ampicillin. In the presence of 50 micrograms of free ampicillin per ml of the incubation medium, intracellular growth of L. monocytogenes was still observed, although less as compared with intracellular growth in the absence of ampicillin. At a concentration of 50 micrograms of free ampicillin plus 100 micrograms of liposome-entrapped ampicillin per ml, 99% of the intracellular bacteria were killed. On the other hand, a concentration of 150 micrograms of free ampicillin per ml plus empty liposomes only inhibited intracellular bacterial growth, and the bacteria were not killed. In addition, empty liposomes at a concentration of 1 mumol of lipid per ml had no effect on intracellular bacterial growth. In broth, liposome-entrapped ampicillin at a concentration of 100 micrograms/ml was not bactericidal for L. monocytogenes, indicating that significant leakage of ampicillin from the liposomes with subsequent killing of the bacteria by the free drug did not occur. Therefore, we concluded that liposomal encapsulation of ampicillin results in an increased availability of the antibiotic for the intracellular bacteria.
机译:通过比较在游离氨苄西林单独或与包裹脂质体的氨苄西林联合存在的情况下,腹膜小鼠巨噬细胞中单核细胞增生李斯特氏菌的存活率,研究了氨苄青霉素脂质体包封对细胞内李斯特菌的抗菌活性的影响。在每毫升温育培养基中存在50微克游离氨苄青霉素的情况下,仍观察到单核细胞增生李斯特氏菌的细胞内生长,尽管与不存在氨苄西林的细胞内生长相比。每毫升浓度为50微克的游离氨苄青霉素加100微克的脂质体包裹的氨苄青霉素,可杀死99%的细胞内细菌。另一方面,每毫升150微克游离氨苄青霉素的浓度加上空脂质体只能抑制细胞内细菌的生长,并且细菌不会被杀死。此外,空脂质体的浓度为每毫升1摩尔摩尔脂质,对细胞内细菌的生长没有影响。在肉汤中,浓度为100微克/毫升的脂质体包裹的氨苄青霉素对单核细胞增生李斯特菌没有杀菌作用,这表明氨苄青霉素从脂质体中大量泄漏并没有随后被游离药物杀死。因此,我们得出的结论是,氨苄西林的脂质体包裹导致细胞内细菌的抗生素利用率增加。

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