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

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Lumen , D , Näkki , S , Imlimthan , S , Lambidis , E , Sarparanta , M , Xu , W , Lehto , V-P & Airaksinen , A J 2019 , ' Site-Specific In-111-Radiolabeling of Dual-PEGylated Porous Silicon Nanoparticles and Their In Vivo Evaluation in Murine 4T1 Breast Cancer Model ' , Pharmaceutics , vol. 11 , no. 12 , 686 . https://doi.org/10.3390/pharmaceutics11120686

Title: Site-Specific In-111-Radiolabeling of Dual-PEGylated Porous Silicon Nanoparticles and Their In Vivo Evaluation in Murine 4T1 Breast Cancer Model
Author: Lumen, Dave; Näkki, Simo; Imlimthan, Surachet; Lambidis, Elisavet; Sarparanta, Mirkka; Xu, Wujun; Lehto, Vesa-Pekka; Airaksinen, Anu J.
Contributor: University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
University of Helsinki, Department of Chemistry
Date: 2019-12
Language: eng
Number of pages: 16
Belongs to series: Pharmaceutics
ISSN: 1999-4923
URI: http://hdl.handle.net/10138/310739
Abstract: 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.
Subject: SPECT
indium-111
click chemistry
porous silicon
IEDDA
DIELS-ALDER REACTIONS
DRUG-DELIVERY
MESOPOROUS SILICON
CLICK CHEMISTRY
ENHANCED PERMEABILITY
PARTICLES
NANOCARRIERS
STABILITY
KINETICS
CARRIER
116 Chemical sciences
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