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Polymers 2011, 3(3), 1107-1125; doi:10.3390/polym3031107
Article

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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Received: 11 June 2011; Accepted: 15 July 2011 / Published: 18 July 2011
(This article belongs to the Special Issue Polymer Nanogels and Microgels)
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Abstract: 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.
Keywords: drug delivery; folate-conjugate nanogel; 5-fluorouracil; culture cells; pharmacokinetic drug delivery; folate-conjugate nanogel; 5-fluorouracil; culture cells; pharmacokinetic
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Blanco, M.D.; Guerrero, S.; Benito, M.; Fernández, A.; Teijón, C.; Olmo, R.; Katime, I.; Teijón, J.M. In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System. Polymers 2011, 3, 1107-1125.

AMA Style

Blanco MD, Guerrero S, Benito M, Fernández A, Teijón C, Olmo R, Katime I, Teijón JM. In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System. Polymers. 2011; 3(3):1107-1125.

Chicago/Turabian Style

Blanco, M. Dolores; Guerrero, Sandra; Benito, Marta; Fernández, Ana; Teijón, César; Olmo, Rosa; Katime, Issa; Teijón, José M. 2011. "In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System." Polymers 3, no. 3: 1107-1125.


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