庆大霉素负载白蛋白微球作为治疗大肠杆菌K88感染的潜在药物载体的制备和表征

A. Sarabia‐Sainz, G. R. Montfort, J. Lizardi‐Mendoza, M. Sánchez‐Saavedra, M. Candia-Plata, R. Guzman, A. Lucero‐Acuña, L. Vázquez-Moreno
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引用次数: 6

摘要

本研究的目的是制定和表征庆大霉素负载白蛋白微球对大肠杆菌K88感染的潜在治疗用途。基于体外实验,提出微球可能作为庆大霉素的载体,在治疗猪大肠杆菌病中具有局部抗菌活性。采用水/油(W/O)乳液与不同浓度的戊二醛交联制备庆大霉素-白蛋白微球(GAM)。电镜显示球形颗粒,有压痕。GAM的平均尺寸为10.5 ~ 12.3µm。在pH为7.2时,庆大霉素从GAM的释放动力学被成功地描述为由一级方程定义的初始爆发。庆大霉素的释放不受戊二醛浓度的影响,但受酸性条件的影响。在pH值为7.2的条件下,胰酶和胰凝乳酶对GAM中庆大霉素的释放行为没有影响。此外,GAM释放的庆大霉素达到抑菌活性的浓度与游离庆大霉素对大肠杆菌K88的浓度相似。这项工作显示了GAM作为庆大霉素治疗载体在猪肠道感染中的潜在应用
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and characterization of gentamicin-loaded albumin microspheres as a potential drug carrier for the treatment of E. coli K88 infections
The aim of this study was to formulate and characterize gentamicin-loaded albumin microspheres for their potential therapeutic use in E. coli K88 infections. Based on in vitro assays, it is proposed that microspheres may serve as a carrier of gentamicin and may provide localized antibacterial activity in the treatment of porcine colibacillosis. Gentamicin-albumin microspheres (GAM) were obtained using a water/oil (W/O) emulsion followed by cross-linking with different concentrations of glutaraldehyde. Electron microscopy showed spherical particles with indentations. The average size of the GAM was 10.5-12.3 µm. At pH 7.2, the release kinetics of gentamicin from the GAM was successfully described as an initial burst defined by a first order equation.  Gentamicin release was unaffected by the glutaraldehyde concentrations used but was affected by acidic conditions.  The behavior of gentamicin release from the GAM was not altered by digestion with trypsin and chymotrypsin at pH 7.2. Additionally, the concentration of gentamicin released from GAM to reach antibacterial activity was similar to that of free gentamicin against E. coli K88. This work shows the potential use of GAM as therapeutic vehicles of gentamicin to counteract intestinal infections in pigs
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