Gold nanoparticles (AuNPs) are among the best candidates for nanomedicines due to their low toxicity, high stability, and ease of modification. An efficient methodology was introduced to prepare maleimide-tethered, water soluble 3nm AuNP. This AuNP core is surrounded by 30 maleimide-terminated ligands and 60 thiolated PEG. This template AuNP exhibits low cytotoxicity (IC50> 0.5mM). Due to the high sensitivity of PET imaging, for each of the maleimide-AuNP, it was necessary to derivatize only 3 maleimide ligands with 18F-SIFA-SH via a Michael addition reaction (radiochemical yield >65%). PET scans of infused rats with these small 18F-AuNPs demonstrated that these AuNPs are capable of crossing the blood brain barrier and accumulate 50% higher than in the background bone and muscle, thus makes it promising for PET brain image. The multiple maleimide sites on the AuNP also offers an opportunity to improve specific binding properties and for application in drug delivery.

Development of a Au nanoparticles template for PET in vivo imaging: <sup>18</sup>F labeled 3nm water-soluble AuNP cross the blood brain barrier

244th National Meeting (2012)

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Development of a Au nanoparticles template for PET in vivo imaging: 18F labeled 3nm water-soluble AuNP cross the blood brain barrier

Development of a Au nanoparticles template for PET in vivo imaging: ¹⁸F labeled 3nm water-soluble AuNP cross the blood brain barrier