Lipid-core nanocapsules restrained the indomethacin ethyl ester hydrolysis in the gastrointestinal lumen and wall acting as mucoadhesive reservoirs
| Autor: | Vitória B. Cattani, Eliézer Jäger, S.S. Guterres, Flávia De Toni Uchôa, Adriana Raffin Pohlmann, Alessandro Jäger, Valter Stefani, Teresa Dalla Costa, Letícia Marques Colomé, Luana Almeida Fiel |
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| Rok vydání: | 2009 |
| Předmět: |
Male
Indomethacin Pharmaceutical Science Lumen (anatomy) Administration Oral Pharmacology Intestinal absorption Nanocapsules Indometacin In vivo Mucoadhesion medicine Animals Tissue Distribution Intestinal Mucosa Rats Wistar Fluorescent Dyes Gastrointestinal tract Drug Carriers Chemistry Hydrolysis Anti-Inflammatory Agents Non-Steroidal Rats Biochemistry Intestinal Absorption Models Animal Tissue Adhesives Ex vivo medicine.drug |
| Zdroj: | European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 39(1-3) |
| ISSN: | 1879-0720 |
| Popis: | The aim of this work was to investigate if the indomethacin ethyl ester (IndOEt) released from lipid-core nanocapsules (NC) is converted into indomethacin (IndOH) in the intestine lumen, intestine wall or after the particles reach the blood stream. NC-IndOEt had monomodal size distribution (242 nm; PDI 0.2) and zeta potential of -11 mV. The everted rat gut sac model showed IndOEt passage of 0.16 micromol m(-2) through the serosal fluid (30 min). From 15 to 120 min, the IndOEt concentrations in the tissue increased from 6.13 to 27.47 micromol m(-2). No IndOH was formed ex vivo. A fluorescent-NC formulation was used to determine the copolymer bioadhesion (0.012 micromol m(-2)). After NC-IndOEt oral administration to rats, IndOEt and IndOH were detected in the gastrointestinal tract (contents and tissues). In the tissues, the IndOEt concentrations decreased from 459 to 5 microg g(-1) after scrapping, demonstrating the NC mucoadhesion. In plasma (peripheric and portal vein), in spleen and liver, exclusively IndOH was detected. In conclusion, after oral dosing of NC-IndOEt, IndOEt is converted into IndOH in the intestinal lumen and wall before reaching the blood stream. The complexity of a living system was not predicted by the ex vivo gut sac model. |
| Databáze: | OpenAIRE |
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