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Published on: February 6, 2016
Multifunctional compact zwitterionic ligands for preparing robust biocompatible semiconductor quantum dots and gold
Kimihiro Susumu1, Eunkeu Oh, James B Delehanty
1Optical Sciences Division, Code 5611, U.S. Naval Research Laboratory, Washington, D.C. 20375, USA. susumu@ccs.nrl.navy.mil
Journal of the American Chemical Society
|May 27, 2011
Summary
New compact ligands create zwitterionic, biocompatible nanoparticles. These functionalized quantum dots (QDs) and gold nanoparticles (AuNPs) show excellent stability, cellular uptake, and in vivo biocompatibility for diverse biological applications.
Area of Science:
- Nanotechnology
- Materials Science
- Biomedical Engineering
Background:
- Developing biocompatible nanomaterials is crucial for advanced biological applications.
- Quantum dots (QDs) and gold nanoparticles (AuNPs) offer unique optical and physical properties but require surface functionalization for biological integration.
- Existing surface ligands often lack the optimal balance of hydrophilicity, biocompatibility, and stability.
Purpose of the Study:
- To synthesize and characterize novel compact ligands for creating hydrophilic, biocompatible quantum dots (QDs) and gold nanoparticles (AuNPs).
- To impart zwitterionic character to nanoparticles for enhanced stability and biological compatibility.
- To evaluate the performance of these functionalized nanoparticles in biological systems, including protein conjugation, cellular uptake, and in vivo applications.
Main Methods:
- Synthesis of four distinct compact ligands featuring a dihydrolipoic acid (DHLA) anchor, tertiary amines, and carboxyl/hydroxyl groups.
- Functionalization of QDs and AuNPs with the synthesized ligands.
- Comprehensive physical characterization of functionalized nanoparticles (surface charge, wettability, hydrodynamic size, pH/salt tolerance).
- Assessment of nanoparticle utility through protein conjugation, covalent coupling, Förster resonance energy transfer (FRET), cellular uptake studies, cytotoxicity assays, and in vivo monitoring.
Main Results:
- Successfully synthesized compact ligands that impart zwitterionic character and hydrophilicity to QDs and AuNPs.
- Functionalized nanoparticles exhibited excellent colloidal stability across a wide pH range and high salt concentrations.
- Ligand-coated QDs demonstrated efficient conjugation to proteins and peptides, facilitated rapid cellular uptake via cell-penetrating peptides, and showed no cytotoxicity.
- In vivo studies confirmed the biocompatibility and stability of the functionalized QDs.
- AuNPs functionalized with the same ligands displayed similar favorable colloidal properties.
Conclusions:
- The novel compact ligands effectively create hydrophilic, biocompatible, and stable QDs and AuNPs.
- These functionalized nanoparticles demonstrate significant potential for diverse biological applications, including bioimaging and drug delivery.
- The ligand design offers a versatile platform for enhancing nanoparticle performance in biological environments.
- The developed nanoparticles show promise for in vitro and in vivo applications with minimal toxicity.

