RT Journal Article T1 In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System A1 Blanco Gaitán, María Dolores A1 Guerrero, Sandra A1 Benito, Marta A1 Fernández Olleros, Ana María A1 Teijón López, César A1 Olmo López, Rosa María A1 Katime, Issa A1 Teijón, José María AB 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. PB MDPI SN 2073-4360 YR 2011 FD 2011-07-18 LK https://hdl.handle.net/20.500.14352/43192 UL https://hdl.handle.net/20.500.14352/43192 LA eng NO Ministerio de Ciencia e Innovación (MICINN) NO Universidad Complutense de Madrid/Comunidad de Madrid DS Docta Complutense RD 23 abr 2025