title: Improved in vitro efficacy of gold nanoconstructs by increased loading of G-quadruplex aptamer.
abstract: This paper describes how in vitro efficacy of aptamer-loaded gold nanostars (Apt-AuNS) can be enhanced by the increased loading of a G-quadruplex homodimer AS1411 (Apt) on the AuNS surface. In a low pH buffer environment, the loading density of Apt on AuNS was increased up to 2.5 times that obtained using the conventional salt-aging process. These highly loaded AuNS nanoconstructs (*Apt-AuNS) were taken up in pancreatic cancer and fibrosarcoma cells ca. 2 times more and at faster rates compared to Apt-AuNS. When a similar number of AuNS carriers was internalized by the cancer cells, the amount of AS1411 delivered via *Apt-AuNS was effectively double that of Apt-AuNS, and *Apt-AuNS resulted in an average of 42% increase in cell death. These results suggest that increasing the loading density on AuNS could provide a simple means to improve uptake as well as in vitro efficacy of the nanoconstructs in cancer cells.
authors.affiliation: Department of Chemistry and ‡Department of Materials Science and Engineering, Northwestern University , 2145 Sheridan Road, Evanston, Illinois 60208, United States.
authors.forename: Duncan Hieu M
authors.initials: DH
authors.lastname: Dam
authors.forename: Raymond C
authors.initials: RC
authors.lastname: Lee
authors.forename: Teri W
authors.initials: TW
authors.lastname: Odom
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D052157:Aptamers, Nucleotide / Q000008:administration & dosage / Q000737:chemistry*; D002460:Cell Line; D045744:Cell Line, Tumor; D004277:DNA, Single-Stranded / Q000737:chemistry; D016503:Drug Delivery Systems; D054856:G-Quadruplexes; D006046:Gold / Q000008:administration & dosage / Q000737:chemistry*; D006801:Humans; D049329:Nanostructures / Q000008:administration & dosage / Q000737:chemistry*; D009841:Oligonucleotides / Q000008:administration & dosage / Q000737:chemistry; D010750:Phosphoproteins / Q000737:chemistry; D016601:RNA-Binding Proteins / Q000737:chemistry; D000097796:Nucleolin
chemical_list: D052157:Aptamers, Nucleotide; D004277:DNA, Single-Stranded; D006046:Gold; D009841:Oligonucleotides; D010750:Phosphoproteins; D016601:RNA-Binding Proteins; D000097796:Nucleolin