Onyeji C O, Nightingale C H, Marangos M N
Dept. of Pharmacy and Research, Hartford Hospital, Connecticut 06115.
Infection. 1994 Sep-Oct;22(5):338-42. doi: 10.1007/BF01715542.
The antibacterial effects of liposomal vancomycin and teicoplanin against intracellular methicillin-resistant Staphylococcus aureus (MRSA) were evaluated using a macrophage infection model. Human blood-derived monocytes were cultured for 7 days to obtain adherent macrophages. Uptake of each drug by macrophages was markedly enhanced by liposomal encapsulation. Following phagocytosis and removal of residual extracellular MRSA, the infected macrophages were exposed to clinically achievable concentrations of teicoplanin and vancomycin. The free (untrapped) and liposome-entrapped forms of each drug were used at the same concentration. The number of intracellular surviving bacteria was determined by colony counts after lysis of the macrophages at different time intervals following drug treatment. Intracellular antimicrobial effect of each drug was significantly (p < 0.001) increased by entrapment in liposomes. Also, the efficacies of the free and liposomal forms of both drugs were correspondingly comparable (p > 0.05). It is, therefore, concluded that liposomal encapsulation of vancomycin and teicoplanin results in an increased availability of the antibiotics for efficient elimination of intracellular MRSA infection.
使用巨噬细胞感染模型评估了脂质体万古霉素和替考拉宁对细胞内耐甲氧西林金黄色葡萄球菌（MRSA）的抗菌作用。将人血来源的单核细胞培养7天以获得贴壁巨噬细胞。脂质体包封显著增强了巨噬细胞对每种药物的摄取。在吞噬并去除残留的细胞外MRSA后，将感染的巨噬细胞暴露于临床可达到的替考拉宁和万古霉素浓度。每种药物的游离（未包封）形式和脂质体包封形式以相同浓度使用。在药物处理后的不同时间间隔裂解巨噬细胞后，通过菌落计数确定细胞内存活细菌的数量。脂质体包封显著（p < 0.001）增强了每种药物的细胞内抗菌作用。此外，两种药物的游离形式和脂质体形式的疗效相应可比（p > 0.05）。因此，得出结论，万古霉素和替考拉宁的脂质体包封导致抗生素的可用性增加，从而有效消除细胞内MRSA感染。
