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Transfer of Lipophilic Markers from PLGA and Polystyrene Nanoparticles to Caco-2 Monolayers Mimics Particle Uptake

Pietzonka, Peter ; Rothen-Rutishauser, Barbara ; Langguth, Peter ; Wunderli-Allenspach, Heidi ; Walter, Elke ; Merkle, Hans

In: Pharmaceutical Research, 2002, vol. 19, no. 5, p. 595-601

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    Title
    • Transfer of Lipophilic Markers from PLGA and Polystyrene Nanoparticles to Caco-2 Monolayers Mimics Particle Uptake
    Author
    • Pietzonka, Peter. Institute of Pharmaceutical Sciences, ETH Zurich, CH-8057, Winterthurerstrasse 190, Zurich
    • Rothen-Rutishauser, Barbara. Institute of Pharmaceutical Sciences, ETH Zurich, CH-8057, Winterthurerstrasse 190, Zurich
    • Langguth, Peter. Institute of Pharmaceutical Technology and Biopharmacy, Johannes-Gutenberg-University, Staudinger Weg 5, D-55099, Mainz
    • Wunderli-Allenspach, Heidi. Institute of Pharmaceutical Sciences, ETH Zurich, CH-8057, Winterthurerstrasse 190, Zurich
    • Walter, Elke. Institute of Pharmaceutical Sciences, ETH Zurich, CH-8057, Winterthurerstrasse 190, Zurich
    • Merkle, Hans. Institute of Pharmaceutical Sciences, ETH Zurich, CH-8057, Winterthurerstrasse 190, Zurich
    Document Type
    • Postprint
    Language
    • English
    Published in
    • Pharmaceutical Research, 2002, vol. 19, no. 5, p. 595-601. Kluwer Academic Publishers-Plenum Publishers
    Other Version
    OAI-PMH Identifier
    • oai:doc.rero.ch:318343
    Summary
    Purpose. The objective of this study was to evaluate nanoparticle uptake by the Caco-2 monolayer model in vitro. Special emphasis was placed on the localization and the quantification of the uptake of fluorescently labeled polystyrene and poly(lactic-co-glycolic acid) (PLGA) nanoparticles. Methods. Intracellular fluorescence was localized by fluorescence and confocal laser scanning microscopy. Particle uptake was quantified either directly, by counting internalized nanoparticles after separation from the Caco-2 monolayers, or indirectly, by extraction of the lipophilic fluorescence marker. In vitro release studies of lipophilic markers from nanoparticles were performed in standard buffer systems and buffer systems supplemented with liposomes. Results. Instead of uptake of polystyrene and PLGA nanoparticles by Caco-2 monolayers an efficient transfer of lipophilic fluorescence markers from nanoparticles into Caco-2 cells with subsequent staining of intracellular lipophilic compartments was observed. Whereas in standard buffer no release of fluorescent marker from polystyrene and PLGA nanoparticles was observed, the release studies using liposome dispersions as receiver revealed an efficient transfer of fluorescent marker into the liposome dispersion. Conclusions. The results suggest that the deceptive particle uptake is caused by a collision-induced process facilitating the transfer of lipophilic fluorescent marker by formation of a complex between the nanoparticles and the biomembranes. Diffusion of the marker within this complex into lipophilic compartments of the cell strongly affects quantitative evaluation of particle uptake