游离与脂质体庆大霉素大鼠肾毒性及抗菌活性的比较评价：生化、分子与组织病理学分析
Comparative evaluation of nephrotoxicity and antibacterial activity of free and liposomal gentamicin in rats: Biochemical, molecular and histopathological analysis.
摘要(中文译文)
庆大霉素是一种广泛使用的氨基糖苷类抗生素，但其临床应用受到剂量依赖性肾毒性的限制。脂质体药物递送系统可在保留抗菌疗效的同时降低毒性。本研究旨在在大鼠模型中比较评价游离庆大霉素与脂质体庆大霉素的肾毒性和抗菌作用。大鼠分为对照组、游离庆大霉素组（FGT；100 mg/kg）和脂质体庆大霉素组（LipGT；100 mg/kg），给药7天。分析肾功能参数、氧化应激生物标志物、促炎细胞因子、肾损伤标志物及基因表达水平。游离庆大霉素显著升高血清BUN和肌酐水平、氧化应激、炎性细胞因子及肾损伤生物标志物。脂质体庆大霉素减轻了这些改变，表现出保护作用。肌酐水平显示部分恢复正常，而BUN表现出不同的反应。脂质体治疗部分恢复了SIRT3表达，但未使PAX2恢复正常。组织病理学结果支持上述结果。抗菌分析显示，对大肠埃希菌的活性得以保留，但对金黄色葡萄球菌的效力降低。脂质体包封减轻了庆大霉素诱导的肾毒性，同时部分维持了抗菌活性，提示这是一种提高药物安全性的有前景的策略。
Abstract
Gentamicin is a widely used aminoglycoside antibiotic; however, its clinical use is limited by dose-dependent nephrotoxicity. Liposomal drug delivery systems may reduce toxicity while preserving antibacterial efficacy. This study aimed to comparatively evaluate the nephrotoxic and antimicrobial effects of free and liposomal gentamicin in a rat model. Rats were divided into control, free gentamicin (FGT; 100 mg/kg), and liposomal gentamicin (LipGT; 100 mg/kg) groups administered for 7 days. Renal function parameters, oxidative stress biomarkers, pro-inflammatory cytokines, renal injury markers, and gene expression levels were analyzed. Free gentamicin significantly increased serum BUN and creatinine levels, oxidative stress, inflammatory cytokines, and renal injury biomarkers. Liposomal gentamicin attenuated these alterations, demonstrating a protective effect. Creatinine levels showed partial normalization, whereas BUN exhibited a distinct response. Liposomal treatment partially restored SIRT3 expression but did not normalize PAX2. Histopathological findings supported these results. Antimicrobial analysis revealed preserved activity against Escherichia coli but reduced efficacy against Staphylococcus aureus. Liposomal encapsulation mitigates gentamicin-induced nephrotoxicity while partially maintaining antibacterial activity, suggesting a promising strategy to improve drug safety.
如何引用
AMA
Murat Celebi, Hasan Susar, Cagla Celebi, Ozhan Karatas, Orkun Babacan, Izzet Karahan. Comparative evaluation of nephrotoxicity and antibacterial activity of free and liposomal gentamicin in rats: Biochemical, molecular and histopathological analysis.. Journal of liposome research. 2026; doi:10.1080/08982104.2026.2715627.
APA
Murat Celebi, Hasan Susar, Cagla Celebi, Ozhan Karatas, Orkun Babacan, Izzet Karahan (2026). Comparative evaluation of nephrotoxicity and antibacterial activity of free and liposomal gentamicin in rats: Biochemical, molecular and histopathological analysis.. Journal of liposome research. https://doi.org/10.1080/08982104.2026.2715627
GB/T 7714
Murat Celebi, Hasan Susar, Cagla Celebi, Ozhan Karatas, Orkun Babacan, Izzet Karahan. Comparative evaluation of nephrotoxicity and antibacterial activity of free and liposomal gentamicin in rats: Biochemical, molecular and histopathological analysis.[J]. Journal of liposome research, 2026 doi:10.1080/08982104.2026.2715627.
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