Site-Specific 111In-Radiolabeling of Dual-PEGylated Porous Silicon Nanoparticles and Their In Vivo Evaluation in Murine 4T1 Breast Cancer Model

Polyethylene glycol (PEG) has been successfully used for improving circulation time of several nanomaterials but prolonging the circulation of porous silicon nanoparticles (PSi NPs) has remained challenging. Here, we report a site specific radiolabeling of dual-PEGylated thermally oxidized porous si...

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Published in:Pharmaceutics 2019-12, Vol.11 (12), p.686
Main Authors: Lumen, Dave, Näkki, Simo, Imlimthan, Surachet, Lambidis, Elisavet, Sarparanta, Mirkka, Xu, Wujun, Lehto, Vesa-Pekka, Airaksinen, Anu J.
Format: Article
Language:English
Subjects:
Acids
Biocompatibility
Biodegradation
Breast cancer
Ethanol
Nanomaterials
Nanoparticles
Polyethylene glycol
Silicon wafers
Surface chemistry
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Summary:Polyethylene glycol (PEG) has been successfully used for improving circulation time of several nanomaterials but prolonging the circulation of porous silicon nanoparticles (PSi NPs) has remained challenging. Here, we report a site specific radiolabeling of dual-PEGylated thermally oxidized porous silicon (DPEG-TOPSi) NPs and investigation of influence of the PEGylation on blood circulation time of TOPSi NPs. Trans-cyclooctene conjugated DPEG-TOPSi NPs were radiolabeled through a click reaction with [111In]In-DOTA-PEG4-tetrazine (DOTA = 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) and the particle behavior was evaluated in vivo in Balb/c mice bearing 4T1 murine breast cancer allografts. The dual-PEGylation significantly prolonged circulation of [111In]In-DPEG-TOPSi particles when compared to non-PEGylated control particles, yielding 10.8 ± 1.7% of the injected activity/g in blood at 15 min for [111In]In-DPEG-TOPSi NPs. The improved circulation time will be beneficial for the accumulation of targeted DPEG-TOPSi to tumors.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics11120686