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基于聚(马来酸-乙烯基吡咯烷酮)的氨苄西林纳米载药系统的制备、表征及其对耐药菌株的抗菌活性评价。

Development, Characterization, and Antimicrobial Evaluation of Ampicillin-Loaded Nanoparticles Based on Poly(maleic acid--vinylpyrrolidone) on Resistant Strains.

机构信息

Grupo de investigación Biopolimer, Departamento de Farmacia, Facultad de Ciencias Farmacéuticas y Alimentarias, Universidad de Antioquia, Calle 67 No. 53-108, Medellín 050010, Colombia.

Grupo de Investigación Natura, Facultad de Ciencias Naturales, Universidad ICESI, Calle 18 No. 122-135, Cali 760035, Colombia.

出版信息

Molecules. 2022 May 5;27(9):2943. doi: 10.3390/molecules27092943.

Abstract

This study was focused on synthesizing, characterizing, and evaluating the antimicrobial effect of polymer nanoparticles (NPs) loaded with ampicillin. For this, the NPs were produced through polymeric self-assembly in aqueous media assisted by high-intensity sonication, using anionic polymers corresponding to the sodium salts of poly(maleic acid--vinylpyrrolidone) and poly(maleic acid--vinylpyrrolidone) modified with decyl-amine, here named as PMA-VP and PMA-VP-N10, respectively. The polymeric NPs were analyzed and characterized through the formation of polymeric pseudo-phases utilizing pyrene as fluorescent probe, as well as by measurements of particle size, zeta potential, polydispersity index, and encapsulation efficiency. The antimicrobial effect was evaluated by means of the broth microdilution method employing ampicillin sensitive and resistant strains. The results showed that PMA-VP and PMA-VP-N10 polymers can self-assemble, forming several types of hydrophobic pseudo-phases with respect to the medium pH and polymer concentration. Likewise, the results described that zeta potential, particle size, polydispersity index, and encapsulation efficiency are extremely dependent on the medium pH, whereas the antimicrobial activity displayed an interesting recovery of antibiotic activity when ampicillin is loaded in the polymeric NPs.

摘要

本研究专注于合成、表征和评估载有氨苄青霉素的聚合物纳米粒子(NPs)的抗菌效果。为此,通过在高强度超声辅助下在水介质中进行聚合物自组装来生产 NPs,使用相应的阴离子聚合物,即聚(马来酸-乙烯基吡咯烷酮)的钠盐和用癸胺修饰的聚(马来酸-乙烯基吡咯烷酮),分别命名为 PMA-VP 和 PMA-VP-N10。通过利用芘作为荧光探针形成聚合物拟似相等方法对聚合物 NPs 进行分析和表征,以及通过测量粒径、zeta 电位、多分散指数和包封效率。通过采用氨苄青霉素敏感和耐药菌株的肉汤微量稀释法评估抗菌效果。结果表明,PMA-VP 和 PMA-VP-N10 聚合物可以自组装,形成几种类型的相对于介质 pH 和聚合物浓度的疏水性拟似相等。同样,结果表明 zeta 电位、粒径、多分散指数和包封效率极其依赖于介质 pH,而当氨苄青霉素载入聚合物 NPs 时,其显示出有趣的抗生素活性恢复。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f13e/9102852/b9428e874c7f/molecules-27-02943-g001.jpg

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