Next Article in Journal
An Inhalable Theranostic System for Local Tuberculosis Treatment Containing an Isoniazid Loaded Metal Organic Framework Fe-MIL-101-NH2—From Raw MOF to Drug Delivery System
Previous Article in Journal
Repurposing Itraconazole Loaded PLGA Nanoparticles for Improved Antitumor Efficacy in Non-Small Cell Lung Cancers
Previous Article in Special Issue
Controlling and Predicting the Dissolution Kinetics of Thermally Oxidised Mesoporous Silicon Particles: Towards Improved Drug Delivery
Open AccessArticle

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

1
Department of Chemistry, Radiochemistry, University of Helsinki, FI-00014 Helsinki, Finland
2
Department of Applied Physics, University of Eastern Finland, FI-70221 Kuopio, Finland
3
A.I. Virtanen-Institute, Department of Health Sciences, University of Eastern Finland, FI-70221 Kuopio, Finland
4
Turku PET Centre, University of Turku, FI-20521 Turku, Finland
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2019, 11(12), 686; https://doi.org/10.3390/pharmaceutics11120686
Received: 4 November 2019 / Revised: 5 December 2019 / Accepted: 12 December 2019 / Published: 17 December 2019
(This article belongs to the Special Issue Porous Silicon for Drug Delivery)
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. View Full-Text
Keywords: SPECT; indium-111; click chemistry; porous silicon; IEDDA SPECT; indium-111; click chemistry; porous silicon; IEDDA
Show Figures

Graphical abstract

MDPI and ACS Style

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.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop