A1 Refereed original research article in a scientific journal
Site-Specific In-111-Radiolabeling of Dual-PEGylated Porous Silicon Nanoparticles and Their In Vivo Evaluation in Murine 4T1 Breast Cancer Model
Authors: Dave Lumen, Simo Näkki, Surachet Imlimthan, Elisavet Lambidis, Mirkka Sarparanta, Wujun Xu,Vesa-Pekka Lehto, Anu J. Airaksinen
Publisher: MDPI
Publication year: 2019
Journal: Pharmaceutics
Journal name in source: PHARMACEUTICS
Journal acronym: PHARMACEUTICS
Article number: ARTN 686
Volume: 11
Issue: 12
Number of pages: 16
eISSN: 1999-4923
DOI: https://doi.org/10.3390/pharmaceutics11120686
Self-archived copy’s web address: https://research.utu.fi/converis/portal/detail/Publication/45078187
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 [In-111]In-DOTA-PEG(4)-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 [In-111]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 [In-111]In-DPEG-TOPSi NPs. The improved circulation time will be beneficial for the accumulation of targeted DPEG-TOPSi to tumors.
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