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首页> 外文期刊>International Journal of Pharmaceutics >Comparative analysis and properties evaluation of gelatin microspheres crosslinked with glutaraldehyde and 3-glycidoxypropyltrimethoxysilane as drug delivery systems for the antibiotic vancomycin
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Comparative analysis and properties evaluation of gelatin microspheres crosslinked with glutaraldehyde and 3-glycidoxypropyltrimethoxysilane as drug delivery systems for the antibiotic vancomycin

机译:用戊二醛和3烯丙基氧基丙基三甲氧基硅烷交联的明胶微球的比较分析与性能评价作为抗生素万古霉素的药物递送系统

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摘要

In the present comparative study, gelatin microspheres (GMs) were prepared by emulsification-solvent-extraction method using well-known crosslinker: glutaraldehyde (GA) and biocompatible silane-coupling agent glycidoxypropyltrimethoxysilane (GPTMS). Crosslinking with GA was done by a definite and common procedure, while GPTMS crosslinking potency was investigated after 5, 10, 24, and 48 h synthesis periods and the fabrication method was adjusted in order for preparation of GMs with optimized morphological and compositional characteristics. The prepared GMs were then evaluated and compared as drug delivery systems for the antibiotic vancomycin (Vm). Morphological observations, FTIR, ninhydrin assay, swelling behavior evaluation and Hydrolytic degradation analysis proved successful modification of GMs and revealed that increasing synthesis time from 5 h to 24 h and 48 h, when using GPTMS as crosslinker, led to formation of morphologically-optimized GMs with highest crosslinking degree ( similar to 50%) and the slowest hydrolytic degradation rate. Such GMs also exhibited most sustained release period of Vm. The antibacterial test results against gram-positive bacterium Staphylococcus aureus, were in accordance with the release profiles of Vm, as well. Together, GPTMS-crosslinked GMs with their preferable characteristics and known as biocompatible gelatin-siloxane hybrids, could act as proper drug delivery systems for the sustained release of the antibiotic vancomycin.
机译:在本比较研究中,通过使用众所周知的交联剂:戊二醛(GA)和生物相容性硅烷偶联剂丙酸氧基丙基三甲氧基硅烷(GPTMS)制备明胶微球(GMS)制备溶剂溶剂 - 萃取方法。用明确且共同的步骤通过GA交联,而在5,10,24和48小时合成期后研究了GPTMS交联效力,并调节了制造方法以使GMS优化的形态学和组成特征制备。然后评估制备的GMS并将其与用于抗生素万古霉素(VM)的药物递送系统进行比较。形态学观察,FTIR,茚三酮测定,肿胀行为评价和水解降解分析证明了GMS的成功改性,并显示使用GPTM作为交联剂时,将合成时间从5小时增加到24小时,48小时,导致形成形态学优化的GMS具有最高的交联度(类似于50%)和最慢的水解降解速率。这种GMS还表现出VM的最持续释放时期。对革兰氏阳性细菌金黄色葡萄球菌的抗菌试验结果均按照VM的释放轮廓。在一起,具有其优选特性和称为生物相容性明胶 - 硅氧烷杂种的GPTMS-交联的GMS可以充当抗生素万古霉素的持续释放的适当药物递送系统。

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