Investigation of the Cellular Effects of Beta- Cyclodextrin Derivatives on Caco-2 Intestinal Epithelial Cells

Bibliographic Details
Title: Investigation of the Cellular Effects of Beta- Cyclodextrin Derivatives on Caco-2 Intestinal Epithelial Cells
Authors: Ágnes Rusznyák, Milo Malanga, Éva Fenyvesi, Lajos Szente, Judit Váradi, Ildikó Bácskay, Miklós Vecsernyés, Gábor Vasvári, Ádám Haimhoffer, Pálma Fehér, Zoltán Ujhelyi, Béla Nagy Jr., Zsolt Fejes, Ferenc Fenyvesi
Source: Pharmaceutics, Vol 13, Iss 2, p 157 (2021)
Publisher Information: MDPI AG, 2021.
Publication Year: 2021
Collection: LCC:Pharmacy and materia medica
Subject Terms: cyclodextrins, endocystosis, NF-κB, autophagy, lysosomes, Pharmacy and materia medica, RS1-441
More Details: Cyclodextrins are widely used excipients for increasing water-solubility, delivery and bioavailability of lipophilic drugs. By using fluorescent cyclodextrin derivatives, we showed previously that cyclodextrins are able to enter Caco-2 intestinal cells by endocytosis, but the influence of different fluorescent labeling on the same cyclodextrin derivative has not been studied. The consequences of the cellular internalization of cyclodextrins have not been revealed yet either. The aims of this study were to compare the cellular internalization of fluorescein- and rhodamine-labeled (2-hydroxypropyl)-, (HPBCD) and randommethyl-β-cyclodextrins (RAMEB) and to investigate the intracellular effects of these derivatives on Caco-2 cells. Stimulation of the NF-kappa B pathway and autophagy and localization of these derivatives in lysosomes were tested. The endocytosis of these derivatives was examined by fluorescence microscopy and flow cytometry. Both fluorescein- and rhodamine-labeled derivatives entered the cells, therefore the type of the fluorescent labeling did not influence their internalization. Cyclodextrin pretreatment did not activate the translocation of the p65 subunit of the NF-kappa B heterodimer into the cell nuclei from the cytoplasm. After HPBCD or RAMEB treatment, formation of the autophagosomes did not increase compared to the control sample and at the same time these derivatives could be detected in lysosomes after internalization.
Document Type: article
File Description: electronic resource
Language: English
ISSN: 1999-4923
Relation: https://www.mdpi.com/1999-4923/13/2/157; https://doaj.org/toc/1999-4923
DOI: 10.3390/pharmaceutics13020157
Access URL: https://doaj.org/article/7b372b13e05148948057cf688fe5c552
Accession Number: edsdoj.7b372b13e05148948057cf688fe5c552
Database: Directory of Open Access Journals
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More Details
ISSN:19994923
DOI:10.3390/pharmaceutics13020157
Published in:Pharmaceutics
Language:English