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(99m)Tc-labelled nanosystem as tumour imaging agent for SPECT and SPECT/CT modalities.

Abstract：

:We report the synthesis, in vitro and in vivo investigation of folate-targeted, biocompatible, biodegradable self-assembled nanoparticles radiolabelled with (99m)Tc, as potential new SPECT or SPECT/CT imaging agent. Nanoparticles with hydrodynamic size in the range of 75-200 nm were prepared by self-assembly of chitosan and folated poly-γ-glutamic acid, and then radiolabelled with (99m)Tc. The nanoparticles target tumour cells overexpressing folate receptors and internalize specifically into them to realize early tumour diagnosis detected by SPECT and SPECT/CT modalities. Rat hepatocellular carcinoma cells were used as model system. Cell specificity and tumour targeting efficacy of these nanosystems were investigated in vitro, and in vivo using SPECT and fusion nanoSPECT/CT imaging. In vitro results showed that the radiolabeled nanosystem was efficiently internalized by tumour cells. Whole-body biodistribution of the new radiolabelled, folate-targeted nanoparticles revealed higher uptake in the tumorous kidney compared to the non-tumorous contralateral side. Uptake by the lungs and thyroids was negligible, which confirmed the stability of the nanoparticles in vivo. In vivo SPECT and SPECT/CT imaging visually reinforced the uptake results and were in accordance with the biodistribution data: the new nanoparticles as a targeted contrast agent improve tumour targeting and are able to detect folate-receptor-overexpressing tumours in animal models with enhanced contrast.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Polyák A,Hajdu I,Bodnár M,Trencsényi G,Pöstényi Z,Haász V,Jánoki G,Jánoki GA,Balogh L,Borbély J

doi

10.1016/j.ijpharm.2013.03.049

subject

Has Abstract

pub_date

2013-06-05 00:00:00

pages

10-7

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(13)00268-8

journal_volume

449

pub_type

杂志文章

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