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 organization: Department of Chemistry
Tracers in Molecular Imaging (TRIM)
Helsinki In Vivo Animal Imaging Platform (HAIP)
Date: 2019-12
Language: eng
Number of pages: 16
Belongs to series: Pharmaceutics
ISSN: 1999-4923
DOI: https://doi.org/10.3390/pharmaceutics11120686
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
Peer reviewed: Yes
Rights: cc_by
Usage restriction: openAccess
Self-archived version: publishedVersion


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