Folate-targeted polymeric micelles loaded with ultrasmall superparamagnetic iron oxide: combined small size and high MRI sensitivity

Guo-bin Hong,1,2 Jing-xing Zhou,2 Ren-xu Yuan31Department of Radiology, Fifth Affiliated Hospital, Zhuhai, 2Department of Radiology, Sun Yat-sen Memorial Hospital, Guangzhou, 3School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou, ChinaAbstract: Targeted delivery of contras...

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Autores principales: Hong GB, Zhou JX, Yuan RX
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Publicado: Dove Medical Press 2012
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spelling oai:doaj.org-article:99b090581abd4cbf94304c10902d362d2021-12-02T02:44:05ZFolate-targeted polymeric micelles loaded with ultrasmall superparamagnetic iron oxide: combined small size and high MRI sensitivity1176-91141178-2013https://doaj.org/article/99b090581abd4cbf94304c10902d362d2012-06-01T00:00:00Zhttp://www.dovepress.com/folate-targeted-polymeric-micelles-loaded-with-ultrasmall-superparamag-a10076https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Guo-bin Hong,1,2 Jing-xing Zhou,2 Ren-xu Yuan31Department of Radiology, Fifth Affiliated Hospital, Zhuhai, 2Department of Radiology, Sun Yat-sen Memorial Hospital, Guangzhou, 3School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou, ChinaAbstract: Targeted delivery of contrast agents is a highly desirable strategy for enhancing diagnostic efficiency and reducing side effects and toxicity. Water-soluble and tumor-targeting superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized by loading hydrophobic SPIONs into micelles assembled from an amphiphilic block copolymer poly(ethylene glycol)-poly(ε-caprolactone) (PEG-PCL) bearing folate in the distal ends of PEG chains. Compared to the water-soluble SPIONs obtained by small molecular surfactant coating, ultrasmall SPION encapsulation with PEG-PCL micelles (PEG-PCL-SPIONs) simultaneously increases transverse (r2) and decreases longitudinal (r1) magnetic resonance (MR) relaxivities of water proton in micelle solution, leading to a notably high r2/r1 ratio up to 78, which makes the PEG-PCL-SPIONs a highly sensitive MR imaging (MRI) T2 contrast agent. The mean size of folate-attached SPION micelles (Fa-PEG-PCL-SPIONs) is 44 ± 3 nm on average, ideal for in vivo MRI applications in which long circulation is greatly determined by small particle size and is highly desirable. Prussian blue staining of BEL-7402 cells over-expressing folate receptors, after incubation with micelle-containing medium, demonstrated that folate functionalization of the magnetic particles significantly enhanced their cell uptake. The potential of Fa-PEG-PCL-SPIONs as a potent MRI probe for in vivo tumor detection was assessed. At 3 hours after intravenous injection of the Fa-PEG-PCL-SPION solution into mice bearing subcutaneous xenografts of human BEL-7402 hepatoma, a 41.2% signal intensity decrease was detected in the T2-weighted MR images of the tumor, indicating the efficient accumulation of Fa-PEG-PCL-SPIONs in the tumor tissue.Keywords: tumor targeting, magnetic resonance imaging, polymeric micelles, superparamagnetic iron oxideHong GBZhou JXYuan RXDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 2863-2872 (2012)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Hong GB
Zhou JX
Yuan RX
Folate-targeted polymeric micelles loaded with ultrasmall superparamagnetic iron oxide: combined small size and high MRI sensitivity
description Guo-bin Hong,1,2 Jing-xing Zhou,2 Ren-xu Yuan31Department of Radiology, Fifth Affiliated Hospital, Zhuhai, 2Department of Radiology, Sun Yat-sen Memorial Hospital, Guangzhou, 3School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou, ChinaAbstract: Targeted delivery of contrast agents is a highly desirable strategy for enhancing diagnostic efficiency and reducing side effects and toxicity. Water-soluble and tumor-targeting superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized by loading hydrophobic SPIONs into micelles assembled from an amphiphilic block copolymer poly(ethylene glycol)-poly(ε-caprolactone) (PEG-PCL) bearing folate in the distal ends of PEG chains. Compared to the water-soluble SPIONs obtained by small molecular surfactant coating, ultrasmall SPION encapsulation with PEG-PCL micelles (PEG-PCL-SPIONs) simultaneously increases transverse (r2) and decreases longitudinal (r1) magnetic resonance (MR) relaxivities of water proton in micelle solution, leading to a notably high r2/r1 ratio up to 78, which makes the PEG-PCL-SPIONs a highly sensitive MR imaging (MRI) T2 contrast agent. The mean size of folate-attached SPION micelles (Fa-PEG-PCL-SPIONs) is 44 ± 3 nm on average, ideal for in vivo MRI applications in which long circulation is greatly determined by small particle size and is highly desirable. Prussian blue staining of BEL-7402 cells over-expressing folate receptors, after incubation with micelle-containing medium, demonstrated that folate functionalization of the magnetic particles significantly enhanced their cell uptake. The potential of Fa-PEG-PCL-SPIONs as a potent MRI probe for in vivo tumor detection was assessed. At 3 hours after intravenous injection of the Fa-PEG-PCL-SPION solution into mice bearing subcutaneous xenografts of human BEL-7402 hepatoma, a 41.2% signal intensity decrease was detected in the T2-weighted MR images of the tumor, indicating the efficient accumulation of Fa-PEG-PCL-SPIONs in the tumor tissue.Keywords: tumor targeting, magnetic resonance imaging, polymeric micelles, superparamagnetic iron oxide
format article
author Hong GB
Zhou JX
Yuan RX
author_facet Hong GB
Zhou JX
Yuan RX
author_sort Hong GB
title Folate-targeted polymeric micelles loaded with ultrasmall superparamagnetic iron oxide: combined small size and high MRI sensitivity
title_short Folate-targeted polymeric micelles loaded with ultrasmall superparamagnetic iron oxide: combined small size and high MRI sensitivity
title_full Folate-targeted polymeric micelles loaded with ultrasmall superparamagnetic iron oxide: combined small size and high MRI sensitivity
title_fullStr Folate-targeted polymeric micelles loaded with ultrasmall superparamagnetic iron oxide: combined small size and high MRI sensitivity
title_full_unstemmed Folate-targeted polymeric micelles loaded with ultrasmall superparamagnetic iron oxide: combined small size and high MRI sensitivity
title_sort folate-targeted polymeric micelles loaded with ultrasmall superparamagnetic iron oxide: combined small size and high mri sensitivity
publisher Dove Medical Press
publishDate 2012
url https://doaj.org/article/99b090581abd4cbf94304c10902d362d
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AT zhoujx folatetargetedpolymericmicellesloadedwithultrasmallsuperparamagneticironoxidecombinedsmallsizeandhighmrisensitivity
AT yuanrx folatetargetedpolymericmicellesloadedwithultrasmallsuperparamagneticironoxidecombinedsmallsizeandhighmrisensitivity
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