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用于阿莫西林(一种抗菌药物)持续释放的基于聚合物的纳米颗粒的开发和特性研究。

Development and characterization of polymeric-based nanoparticles for sustained release of amoxicillin - an antimicrobial drug.

机构信息

a Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine , Kırıkkale University , Kırıkkale , Turkey.

b Department of Chemistry, Faculty of Science and Arts , Kırıkkale University , Kırıkkale , Turkey.

出版信息

Artif Cells Nanomed Biotechnol. 2018;46(sup2):964-973. doi: 10.1080/21691401.2018.1476371. Epub 2018 May 26.

DOI:10.1080/21691401.2018.1476371
PMID:29806495
Abstract

In this study, amoxicillin (AMO)-loaded poly(vinyl alcohol)/sodium alginate (PVA/NaAlg) nanoparticles were prepared as a polymer-based controlled release system. The physicochemical properties of the obtained nanoparticles were investigated by XRD, DSC/TGA, particle size analyses and zeta potential measurements. The average particle sizes were in the range from 336.3 ± 25.66 to 558.3 ± 31.39 nm with negative zeta potential values from -41.86 ± 0.55 to -47.3 ± 2.76 mV. The influences of PVA/NaAlg ratio, span 80 concentration, exposure time to glutaraldehyde (GA) and the drug/polymer ratio on AMO release profiles were evaluated. In vitro drug release studies showed a controlled and pH dependent AMO release with an initial burst effect. XRD patterns and DSC thermograms of AMO-loaded nanoparticles revealed that the drug in the nanoparticles was in amorphous form, which was more stable than the crystalline form. The antibacterial activity of the optimal formulation was also investigated. The minimum inhibitory concentration (MIC) values of this formulation had the comparable antibacterial activity with that of pure AMO. These results indicate that the developed nanoparticles could be a promising candidate drug delivery system for AMO.

摘要

在这项研究中,阿莫西林(AMO)负载的聚乙烯醇/海藻酸钠(PVA/NaAlg)纳米粒子被制备为聚合物基控制释放系统。通过 XRD、DSC/TGA、粒度分析和zeta 电位测量研究了所得纳米粒子的物理化学性质。平均粒径范围为 336.3±25.66nm 至 558.3±31.39nm,zeta 电位值为-41.86±0.55mV 至-47.3±2.76mV。评估了 PVA/NaAlg 比、吐温 80 浓度、戊二醛(GA)暴露时间和药物/聚合物比对 AMO 释放曲线的影响。体外药物释放研究表明,AMO 具有控制和 pH 依赖性释放,具有初始突释效应。载 AMO 纳米粒子的 XRD 图谱和 DSC 热图谱表明,纳米粒子中的药物呈无定形状态,比晶形状态更稳定。还研究了最佳配方的抗菌活性。该配方的最小抑菌浓度(MIC)值与纯 AMO 的抗菌活性相当。这些结果表明,所开发的纳米粒子可能是 AMO 的一种有前途的药物递送系统。

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