Endocytosis of fluorescent cyclodextrins by intestinal Caco-2 cells and its role in paclitaxel drug delivery

Katalin Réti-Nagy, Milo Malanga, Éva Fenyvesi, Lajos Szente, György Vámosi, Judit Váradi, Ildikó Bácskay, Pálma Fehér, Zoltán Ujhelyi, Eszter Róka, Miklós Vecsernyés, György Balogh, Gábor Vasvári, Ferenc Fenyvesi

Research output: Article

25 Citations (Scopus)


Cyclodextrins are widely used excipients in pharmaceutical formulations. They are mainly utilized as solubilizers and absorption enhancers, but recent results revealed their effects on cell membranes and pharmacological barriers. In addition to the growing knowledge on their interaction with plasma membranes, it was confirmed that cyclodextrins are able to enter cells by endocytosis. The number of the tested cyclodextrins was limited, and the role of this mechanism in drug absorption and delivery is not known. Our aim was to examine the endocytosis of fluorescently labeled hydroxypropyl-β-cyclodextrin, random methyl-β-cyclodextrin and soluble β-cyclodextrin polymer, and the cellular uptake of the fluorescent paclitaxel derivative-random methyl-β-cyclodextrin complex. The studied cyclodextrin derivatives were able to enter Caco-2 intestinal cells and localized in vesicles in the cytoplasm, while their permeability was very limited through Caco-2 monolayers. We demonstrated for the first time that the fluorescent paclitaxel derivative and rhodamine-labeled random methyl-β-cyclodextrin were detected in the same intracellular vesicles after treating cells with their inclusion complex. These results indicate that the endocytosis of cyclodextrin complexes can contribute to drug absorption processes.

Original languageEnglish
Pages (from-to)509-517
Number of pages9
JournalInternational Journal of Pharmaceutics
Issue number2
Publication statusPublished - dec. 30 2015


ASJC Scopus subject areas

  • Pharmaceutical Science

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