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High-Throughput Screening of Nanoparticle-Stabilizing Ligands:Application to Preparing Antimicrobial Curcumin Nanoparticles by Antisolvent Precipitation

机译:高通量筛选稳定纳米颗粒的配体:在抗溶剂沉淀法制备抗菌姜黄素纳米颗粒中的应用

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摘要

Water-dispersible curcumin nanoparticles were prepared by bottom-up antisolvent precipitation approach. A new high-throughput screening technique was developed for selecting appropriate ligands stabilizing the nanoparticles in aqueous medium and improving their performance. The initial set of twenty-eight potential stabilizing ligands was evaluated based on their capacity to improve curcumin dispersibility in aqueous medium. The performance of four promising ligands(amino acid proline, polyphenol tannic acid, polycation Polyquaternium 10, and neutral polymer polyvinylpyrrolidone) was tested in ultrasound-aided antisolvent precipitation trials. Using the selected stabilizing ligands diminished the average particle size from ca. 1,200 to 170–230 nm, reduced their dispersity, improved stability, and allowed reaching curcumin concentration of up to 1.4 m M in aqueous medium. Storage stability of the aqueous nanodispersions varied from 2 days to 2 weeks, depending on stabilizing ligand. Studying the effects of ionic strength and pH on size and f-potential of the particles suggested that electrostatic forces and hydrophobic interactions could be the major factors affecting their stability. The ligand-protected nanoparticles showed minimal inhibitory concentration of 400 or500 μM toward Escherichia coli. We suggest that the presented screening approach may be useful for preparing nanoparticles of various poorly water-soluble bioactive materials.
机译:通过自下而上的反溶剂沉淀法制备了水分散型姜黄素纳米颗粒。开发了一种新的高通量筛选技术,用于选择稳定纳米粒子在水性介质中并改善其性能的合适配体。基于其改善姜黄素在水性介质中分散性的能力,评估了最初的28种潜在的稳定配体。在超声辅助的抗溶剂沉淀试验中测试了四种有前途的配体(氨基酸脯氨酸,多酚鞣酸,聚阳离子聚季铵盐10和中性聚合物聚乙烯吡咯烷酮)的性能。使用选择的稳定配体使平均粒径从约3μm减小到约1μm。 1,200至170–230 nm,降低了它们的分散性,提高了稳定性,并使水性介质中的姜黄素浓度达到1.4 mM。取决于稳定的配体,水性纳米分散体的储存稳定性从2天到2周不等。研究离子强度和pH对颗粒尺寸和f-电势的影响表明,静电力和疏水相互作用可能是影响其稳定性的主要因素。配体保护的纳米颗粒显示出对大肠杆菌的最小抑制浓度为400或500μM。我们建议,提出的筛选方法可能对制备各种水溶性差的生物活性物质的纳米颗粒有用。

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