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In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System

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dc.creator M. Dolores Blanco
dc.creator Sandra Guerrero
dc.creator Marta Benito
dc.creator Ana Fernández
dc.creator César Teijón
dc.creator Rosa Olmo
dc.creator Issa Katime
dc.creator José M. Teijón
dc.date 2011
dc.date.accessioned 2013-05-30T11:48:09Z
dc.date.available 2013-05-30T11:48:09Z
dc.date.issued 2013-05-30
dc.identifier http://www.mdpi.com/2073-4360/3/3/1107/
dc.identifier http://www.doaj.org/doaj?func=openurl&genre=article&issn=20734360&date=2011&volume=3&issue=3&spage=1107
dc.identifier.uri http://koha.mediu.edu.my:8181/jspui/handle/123456789/4824
dc.description Folate-targeted poly[(p-nitrophenyl acrylate)-co-(N-isopropylacrylamide)] nanohydrogel (F-SubMG) was loaded with 5-fluorouracil (5-FU) to obtain low (16.3 ± 1.9 μg 5-FU/mg F-SubMG) and high (46.8 ± 3.8 μg 5-FU/mg F-SubMG) load 5-FU-loaded F-SubMGs. The complete in vitro drug release took place in 8 h. The cytotoxicity of unloaded F-SubMGs in MCF7 and HeLa cells was low; although it increased for high F-SubMG concentration. The administration of 10 μM 5-FU by 5-FU-loaded F-SubMGs was effective on both cellular types. Cell uptake of F-SubMGs took place in both cell types, but it was higher in HeLa cells because they are folate receptor positive. After subcutaneous administration (28 mg 5-FU/kg b.w.) in Wistar rats, F-SubMGs were detected at the site of injection under the skin. Histological studies indicated that the F-SubMGs were surrounded by connective tissue, without any signs of rejections, even 60 days after injection. Pharmacokinetic study showed an increase in MRT (mean residence time) of 5-FU when the drug was administered by drug-loaded F-SubMGs.
dc.language eng
dc.publisher Molecular Diversity Preservation International
dc.source Polymers
dc.subject drug delivery
dc.subject folate-conjugate nanogel
dc.subject 5-fluorouracil
dc.subject culture cells
dc.subject pharmacokinetic
dc.title In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System


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