Synthesis and biodistribution of oligonucleotide-functionalized, tumor-targetable carbon nanotubes Journal Article


Authors: Villa, C. H.; McDevitt, M. R.; Escorcia, F. E.; Rey, D. A.; Bergkvist, M.; Batt, C. A.; Scheinberg, D. A.
Article Title: Synthesis and biodistribution of oligonucleotide-functionalized, tumor-targetable carbon nanotubes
Abstract: Single-wall carbon nanotubes (SWNT) show promise as nanoscale vehicles for targeted therapies. We have functionalized SWNT using regioselective chemistries to confer capabilities of selective targeting using RGD ligands, radiotracing using radiometal chelates, and self-assembly using oligonucleotides. The constructs contained approximately 2-7 phosphorothioate oligonucleotide chains and 50-75 amines per 100 nm length of SWNT, based on a loading of 0.01-0.05 mmol/g and 0.3-0.6 mmol/g, respectively. Dynamic light scattering suggested the functionalized SWNT were well dispersed, without formation of large aggregates in physiologic solutions. The SWNT-oligonucleotide conjugate annealed with a complementary oligonucleotide sequence had a melting temperature of 54 °C. Biodistribution in mice was quantified using radiolabeled SWNT-oligonucleotide conjugates. Appended RGD ligands allowed for specific binding to tumor cells in a flow cytometric assay. The techniques employed should enable the synthesis of multifunctional SWNT capable of self-assembly in biological settings. © 2008 American Chemical Society.
Keywords: neoplasm; neoplasms; metabolism; pathology; drug delivery systems; chemistry; amines; tissue distribution; tumors; ligands; bio distributions; nucleic acid hybridization; oligonucleotide; synthesis (chemical); drug delivery system; chromatography, gel; functionalized; oligonucleotides; tumor cells; sugar (sucrose); self assembly; carbon nanotube; nanotubes, carbon; carbon nanotubes; single-wall carbon nanotubes; single-walled carbon nanotubes (swcn); biological settings; functionalized swnt; large aggregates; melting temperatures; nano-scale; oligonucleotide conjugates; oligonucleotide sequences; phosphorothioate oligonucleotides; radiometal chelates; regio-selective; self- assemblies; specific bindings; well-dispersed; melting point; gel chromatography
Journal Title: Nano Letters
Volume: 8
Issue: 12
ISSN: 1530-6984
Publisher: American Chemical Society  
Date Published: 2008-12-01
Start Page: 4221
End Page: 4228
Language: English
DOI: 10.1021/nl801878d
PUBMED: 19367842
PROVIDER: scopus
PMCID: PMC4059415
DOI/URL:
Notes: --- - "Cited By (since 1996): 15" - "Export Date: 17 November 2011" - "Source: Scopus"
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  1. Michael R Mcdevitt
    144 Mcdevitt
  2. Carlos H Villa
    13 Villa