The effect of sucrose esters on a culture model of the nasal barrier

Levente Kürti, S. Veszelka, Alexandra Bocsik, Ngo Thi Khue Dung, Béla Ózsvári, L. Puskás, A. Kittel, P. Szabó-Révész, M. Deli

Research output: Contribution to journalArticle

38 Citations (Scopus)

Abstract

Sucrose esters are effective solubilizers and there is an interest to use them as pharmaceutical excipients for nasal drug delivery. We have determined for the first time the non-toxic doses of laurate and myristate sucrose esters by four independent methods, and their effects on epithelial permeability using RPMI 2650 human nasal epithelial cell line. Based on real-time cell electronic sensing, MTT dye conversion and lactate dehydrogenase release methods reference surfactant Cremophor RH40 proved to be the least toxic excipient, and could be used at 5. mg/mL concentration for 1. h in epithelial cells without cellular damage. The non-toxic dose of Tween 80 was 1. mg/mL, while the dose of laurate and myristate sucrose esters that could be safely used on cells for 1. h was 0.1. mg/mL. Both the reference surfactants and the sucrose esters significantly enhanced the permeability of epithelial cell layers for the paracellular marker FITC-labelled 4.4. kDa dextran at 0.1. mg/mL concentration. The effects of sucrose esters on epithelial permeability were dose-dependent. These data indicate that laurate and myristate sucrose esters can be potentially used as permeability enhancers in nasal formulations to augment drug delivery to the systemic circulation.

Original languageEnglish
Pages (from-to)445-454
Number of pages10
JournalToxicology in Vitro
Volume26
Issue number3
DOIs
Publication statusPublished - Apr 2012

Fingerprint

sucrose monolaurate
Nose
Sucrose
Esters
Permeability
Excipients
Epithelial Cells
Drug delivery
Surface-Active Agents
Pharmaceutical Preparations
Polysorbates
Fluorescein-5-isothiocyanate
Poisons
Dextrans
L-Lactate Dehydrogenase
Coloring Agents
Cell Line
sucrose myristate

Keywords

  • Cell electronic sensing
  • Cytotoxicity
  • Epithelial permeability
  • Human nasal epithelial cell
  • RPMI 2650 cell line
  • Sucrose ester

ASJC Scopus subject areas

  • Toxicology

Cite this

The effect of sucrose esters on a culture model of the nasal barrier. / Kürti, Levente; Veszelka, S.; Bocsik, Alexandra; Dung, Ngo Thi Khue; Ózsvári, Béla; Puskás, L.; Kittel, A.; Szabó-Révész, P.; Deli, M.

In: Toxicology in Vitro, Vol. 26, No. 3, 04.2012, p. 445-454.

Research output: Contribution to journalArticle

Kürti, Levente ; Veszelka, S. ; Bocsik, Alexandra ; Dung, Ngo Thi Khue ; Ózsvári, Béla ; Puskás, L. ; Kittel, A. ; Szabó-Révész, P. ; Deli, M. / The effect of sucrose esters on a culture model of the nasal barrier. In: Toxicology in Vitro. 2012 ; Vol. 26, No. 3. pp. 445-454.
@article{2e24c8f7f95047c3b5a7d989cb47c4e1,
title = "The effect of sucrose esters on a culture model of the nasal barrier",
abstract = "Sucrose esters are effective solubilizers and there is an interest to use them as pharmaceutical excipients for nasal drug delivery. We have determined for the first time the non-toxic doses of laurate and myristate sucrose esters by four independent methods, and their effects on epithelial permeability using RPMI 2650 human nasal epithelial cell line. Based on real-time cell electronic sensing, MTT dye conversion and lactate dehydrogenase release methods reference surfactant Cremophor RH40 proved to be the least toxic excipient, and could be used at 5. mg/mL concentration for 1. h in epithelial cells without cellular damage. The non-toxic dose of Tween 80 was 1. mg/mL, while the dose of laurate and myristate sucrose esters that could be safely used on cells for 1. h was 0.1. mg/mL. Both the reference surfactants and the sucrose esters significantly enhanced the permeability of epithelial cell layers for the paracellular marker FITC-labelled 4.4. kDa dextran at 0.1. mg/mL concentration. The effects of sucrose esters on epithelial permeability were dose-dependent. These data indicate that laurate and myristate sucrose esters can be potentially used as permeability enhancers in nasal formulations to augment drug delivery to the systemic circulation.",
keywords = "Cell electronic sensing, Cytotoxicity, Epithelial permeability, Human nasal epithelial cell, RPMI 2650 cell line, Sucrose ester",
author = "Levente K{\"u}rti and S. Veszelka and Alexandra Bocsik and Dung, {Ngo Thi Khue} and B{\'e}la {\'O}zsv{\'a}ri and L. Pusk{\'a}s and A. Kittel and P. Szab{\'o}-R{\'e}v{\'e}sz and M. Deli",
year = "2012",
month = "4",
doi = "10.1016/j.tiv.2012.01.015",
language = "English",
volume = "26",
pages = "445--454",
journal = "Toxicology in Vitro",
issn = "0887-2333",
publisher = "Elsevier Limited",
number = "3",

}

TY - JOUR

T1 - The effect of sucrose esters on a culture model of the nasal barrier

AU - Kürti, Levente

AU - Veszelka, S.

AU - Bocsik, Alexandra

AU - Dung, Ngo Thi Khue

AU - Ózsvári, Béla

AU - Puskás, L.

AU - Kittel, A.

AU - Szabó-Révész, P.

AU - Deli, M.

PY - 2012/4

Y1 - 2012/4

N2 - Sucrose esters are effective solubilizers and there is an interest to use them as pharmaceutical excipients for nasal drug delivery. We have determined for the first time the non-toxic doses of laurate and myristate sucrose esters by four independent methods, and their effects on epithelial permeability using RPMI 2650 human nasal epithelial cell line. Based on real-time cell electronic sensing, MTT dye conversion and lactate dehydrogenase release methods reference surfactant Cremophor RH40 proved to be the least toxic excipient, and could be used at 5. mg/mL concentration for 1. h in epithelial cells without cellular damage. The non-toxic dose of Tween 80 was 1. mg/mL, while the dose of laurate and myristate sucrose esters that could be safely used on cells for 1. h was 0.1. mg/mL. Both the reference surfactants and the sucrose esters significantly enhanced the permeability of epithelial cell layers for the paracellular marker FITC-labelled 4.4. kDa dextran at 0.1. mg/mL concentration. The effects of sucrose esters on epithelial permeability were dose-dependent. These data indicate that laurate and myristate sucrose esters can be potentially used as permeability enhancers in nasal formulations to augment drug delivery to the systemic circulation.

AB - Sucrose esters are effective solubilizers and there is an interest to use them as pharmaceutical excipients for nasal drug delivery. We have determined for the first time the non-toxic doses of laurate and myristate sucrose esters by four independent methods, and their effects on epithelial permeability using RPMI 2650 human nasal epithelial cell line. Based on real-time cell electronic sensing, MTT dye conversion and lactate dehydrogenase release methods reference surfactant Cremophor RH40 proved to be the least toxic excipient, and could be used at 5. mg/mL concentration for 1. h in epithelial cells without cellular damage. The non-toxic dose of Tween 80 was 1. mg/mL, while the dose of laurate and myristate sucrose esters that could be safely used on cells for 1. h was 0.1. mg/mL. Both the reference surfactants and the sucrose esters significantly enhanced the permeability of epithelial cell layers for the paracellular marker FITC-labelled 4.4. kDa dextran at 0.1. mg/mL concentration. The effects of sucrose esters on epithelial permeability were dose-dependent. These data indicate that laurate and myristate sucrose esters can be potentially used as permeability enhancers in nasal formulations to augment drug delivery to the systemic circulation.

KW - Cell electronic sensing

KW - Cytotoxicity

KW - Epithelial permeability

KW - Human nasal epithelial cell

KW - RPMI 2650 cell line

KW - Sucrose ester

UR - http://www.scopus.com/inward/record.url?scp=84857692132&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84857692132&partnerID=8YFLogxK

U2 - 10.1016/j.tiv.2012.01.015

DO - 10.1016/j.tiv.2012.01.015

M3 - Article

C2 - 22274662

AN - SCOPUS:84857692132

VL - 26

SP - 445

EP - 454

JO - Toxicology in Vitro

JF - Toxicology in Vitro

SN - 0887-2333

IS - 3

ER -