Nano-Micro Letters

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

Ilya Shlar1,2, Elena Poverenov1, Yakov Vinokur1, Batia Horev1, Samir Droby1, Victor Rodov1,*

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Nano-Micro Letters, , Volume 7, Issue 1, pp 68-79

First Online: November 22, 2014 (Article)





Scheme of the high-throughput screening assay.

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. 1200 to 170-230 nm, reduced their dispersity, improved stability and allowed reaching curcumin concentration of up to 1.4 mM in aqueous medium. Storage stability of the aqueous nanodispersions varied from two days to two weeks, depending on stabilizing ligand. Studying the effects of ionic strength and pH on size and ζ-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 (MIC) of 400 or 500 µM towards Escherichia coli. We suggest that the presented screening approach may be useful for preparing nanoparticles of various poorly water-soluble bioactive materials.

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