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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Blanco Gaitán, María Dolores and Guerrero, Sandra and Benito, Marta and Fernández Olleros, Ana María and Teijón López, Cesar and Olmo López, Rosa María and Katime, Issa and Teijón, José María (2011) In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System. Polymers, 3 (3). pp. 1107-1125. ISSN 2073-4360

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Official URL: https://doi.org/10.3390/polym3031107




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.


Item Type:Article
Uncontrolled Keywords:drug delivery; folate-conjugate nanogel; 5-fluorouracil; culture cells; pharmacokinetic
Subjects:Medical sciences > Medicine > Biochemistry
Medical sciences > Medicine > Gynecology and Obstetrics
ID Code:65911
Deposited On:01 Jun 2021 14:22
Last Modified:02 Jun 2021 07:12

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