Abstract
Purpose. The Caco-2 association of lectin-grafted PLGA-nanospheres was investigated compared to plain and BSA-coated spheres.
Methods. Nanospheres made from fluorescent-labeled PLGA were coated with wheat germ agglutinin (WGA) or BSA and incubated with Caco-2 monolayers varying the concentration of nanospheres, the time, and the temperature. The tests were performed in a static horizontal as well as an aerated vertical setup to find out the system most appropriate for estimation of bioadhesion.
Results. Due to bioadhesive effects, WGA-modified particles exhibited highest association to the cells as compared to plain and BSA-coated ones. The amount of associated spheres increased with time and concentration of the nanosphere suspension. Whereas the binding of lectin-coated spheres was independent from energy, their uptake was energy consuming as opposed to BSA and plain nanospheres, which exhibited nonspecific, energy independent binding and uptake. Although more particles were associated with the monolayer in the horizontal setup than in the vertical system, the vertical system reflects true bioadhesion due to circulation of the spheres which inhibits the influence of sedimentation.
Conclusions. Immobilization of WGA considerably enhances the binding as well as the uptake of PLGA-nanospheres by Caco-2 monolayers. For bioadhesion studies, the vertical setup is recommended instead of the horizontal setup.
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Weissenboeck, A., Bogner, E., Wirth, M. et al. Binding and Uptake of Wheat Germ Agglutinin-Grafted PLGA-Nanospheres by Caco-2 Monolayers. Pharm Res 21, 1917–1923 (2004). https://doi.org/10.1023/B:PHAM.0000045247.09724.26
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DOI: https://doi.org/10.1023/B:PHAM.0000045247.09724.26