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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 (242nm; PDI 0.2) and zeta potential of −11mV. The everted rat gut sac model showed IndOEt passage of 0.16μmolm⁻² through the serosal fluid (30min). From 15 to 120min, the IndOEt concentrations in the tissue increased from 6.13 to 27.47μmolm⁻². No IndOH was formed ex vivo. A fluorescent-NC formulation was used to determine the copolymer bioadhesion (0.012μmolm⁻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 5μgg⁻¹ after scrapping, demonstrating the NC …