Cytotoxicity of Different Excipients on RPMI 2650 Human Nasal Epithelial Cells

Horváth, Tamás; Bartos, Csilla; Bocsik, Alexandra; Kiss, Lóránd; Veszelka, Szilvia; Deli, Mária A.; Ujhelyi, Gabriella; Szabó‐Révész, Piroska; Ambrus, Rita

doi:10.3390/molecules21050658

Cited by 17 publications

(12 citation statements)

References 15 publications

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“…Our primary objective, in fact, was to demonstrate the biocompatibility of cationic beta-cyclodextrin monomers and polymers and thus suggesting their use for nasal formulations. All cationic beta-cyclodextrin polymers, QAPS and HAPS, show dose- and time-dependent toxicity; nevertheless, at 5 µM concentration and 60 min of exposure, the cell viability value is about 80% for QAPS and thus it could be recognized as nontoxic [ 24 , 25 , 26 ]. HAPS has low toxic effect at 5 µM concentration and 60 min of exposition.…”

Section: Discussionmentioning

confidence: 99%

Investigation of Cytotoxicity and Cell Uptake of Cationic Beta-Cyclodextrins as Valid Tools in Nasal Delivery

et al. 2020

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Cyclodextrin polymers have high applicability in pharmaceutical formulations due to better biocompatibility, solubility enhancement, loading capacity and controlled drug release than their parent, cyclodextrins. The cytotoxicity and cell uptake of new cationic beta-cyclodextrin monomers and polymers were evaluated as suitable materials for nasal formulations and their protective effects on cells exposed to hydrogen peroxide were studied. PC12 and CACO-2 cells were selected as the neuronal- and epithelial-type cells, respectively, to mimic the structure of respiratory and olfactory epithelia of the nasal cavity. All cationic beta-cyclodextrin polymers tested showed dose- and time-dependent toxicity; nevertheless, at 5 µM concentration and 60 min of exposure, the quaternary-ammonium-beta-cyclodextrin soluble polymer could be recognized as nontoxic. Based on these results, a fluorescently labelled quaternary-ammonium-beta-cyclodextrin monomer and polymer were selected for uptake studies in CACO-2 cells. The monomeric and polymeric beta-cyclodextrins were internalized in the cytoplasm of CACO-2 cells; the cationic monomer showed higher permeability than the hydroxypropyl-beta-cyclodextrin, employed as comparison. Therefore, these cationic beta-cyclodextrins showed potential as excipients able to improve the nasal absorption of drugs. Furthermore, amino-beta-cyclodextrin and beta-cyclodextrin soluble polymers were able to reduce oxidative damage in PC12 and CACO-2 cells and thus could be studied as bioactive carriers or potential drugs for cell protection against oxidative stress.

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Section: Discussionmentioning

confidence: 99%

Investigation of Cytotoxicity and Cell Uptake of Cationic Beta-Cyclodextrins as Valid Tools in Nasal Delivery

et al. 2020

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show abstract

“…Our primary objective, in fact, was to demonstrate the biocompatibility of cationic beta-cyclodextrin monomers and polymers and thus suggesting their use for nasal formulations. All cationic beta-cyclodextrin polymers, QAPS and HAPS, show dose-and time-dependent toxicity; nevertheless, at 5 µ M concentration and 60 min of exposure, the cell viability value is about 80% for QAPS and thus it could be recognized as non-toxic [24][25][26]. HAPS has low toxic effect at 5 µ M concentration and 60 min of exposition.…”

Section: Discussionmentioning

confidence: 99%

Investigation of Cytotoxicity and Cell Uptake of Cationic Beta-Cyclodextrins as Valid Tools in Nasal Delivery

Rassu¹,

Fancello²,

Roldo³

et al. 2020

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Cyclodextrin polymers have high applicability in pharmaceutical formulations due to better biocompatibility, solubility enhancement, loading capacity and controlled drug release than parent the cyclodextrins. The cytotoxicity and cell uptake of new cationic beta-cyclodextrin monomers and polymers were evaluated as suitable material for nasal formulations and their protective effects on cells exposed to hydrogen peroxide were studied. PC12 and CACO-2 cells were selected as the neuronal and epithelial type cells, respectively, to mimic the structure of respiratory and olfactory epithelia of the nasal cavity. All cationic beta-cyclodextrin polymers tested showed dose- and time-dependent toxicity; nevertheless, at 5 µM concentration and 60 min of exposure, the quaternary-ammonium-beta-cyclodextrin soluble polymer could be recognized as non-toxic. Based on these results, fluorescently labelled quaternary-ammonium-beta-cyclodextrin monomer and polymer were selected for uptake studies in CACO-2 cells. The monomeric and polymeric beta-cyclodextrins were internalized in the cytoplasm of CACO-2 cells; the cationic monomer showed higher permeability than the hydroxypropyl-beta-cyclodextrin, employed as comparison. Therefore, these cationic beta-cyclodextrins showed potential as excipients able to improve the nasal absorption of drugs. Furthermore, amino-beta-cyclodextrin and beta-cyclodextrin soluble polymers were able to reduce oxidative damage in PC12 and CACO-2 cells and thus could be studied as bioactive carriers or potential drugs for cells protection against oxidative stress.

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“…Rita Ambrus and coworkers studied the cytotoxicity of six pharmaceutical excipients, which could help to reach larger residence time, better permeability, and an increased solubility dissolution rate. As described in the communication entitled “Cytotoxicity of Different Excipients on RPMI 2650 Human Nasal Epithelial Cells” [ 11 ], they found that all additives at 0.3% sodium hyaluronate and polyvinyl alcohol at 1% concentrations can be safely used for nasal formulations.…”

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confidence: 99%