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

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http://hdl.handle.net/10138/308693

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Lumen, D.; Näkki, S.; Imlimthan, S.; Lambidis, E.; Sarparanta, M.; Xu, W.; Lehto, V.-P.; Airaksinen, A.J. Site-Specific 111In-Radiolabeling of Dual-PEGylated Porous Silicon Nanoparticles and Their In Vivo Evaluation in Murine 4T1 Breast Cancer Model. Pharmaceutics 2019, 11, 686.

Titel: Site-Specific 111In-Radiolabeling of Dual-PEGylated Porous Silicon Nanoparticles and Their In Vivo Evaluation in Murine 4T1 Breast Cancer Model
Författare: Lumen, Dave; Näkki, Simo; Imlimthan, Surachet; Lambidis, Elisavet; Sarparanta, Mirkka; Xu, Wujun; Lehto, Vesa-Pekka; Airaksinen, Anu J.
Utgivare: Multidisciplinary Digital Publishing Institute
Datum: 2019-12-17
Permanenta länken (URI): http://hdl.handle.net/10138/308693
Abstrakt: 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. <i>Trans</i>-cyclooctene conjugated DPEG-TOPSi NPs were radiolabeled through a click reaction with [<sup>111</sup>In]In-DOTA-PEG<sub>4</sub>-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 [<sup>111</sup>In]In-DPEG-TOPSi particles when compared to non-PEGylated control particles, yielding 10.8 &plusmn; 1.7% of the injected activity/g in blood at 15 min for [<sup>111</sup>In]In-DPEG-TOPSi NPs. The improved circulation time will be beneficial for the accumulation of targeted DPEG-TOPSi to tumors.


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