Mucus can change the permeation rank order of drug candidates

Department of Drug Design and Pharmacology

Mucus can change the permeation rank order of drug candidates

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Mucus can change the permeation rank order of drug candidates. / Hagesaether, Ellen; Christiansen, Elisabeth; Due-Hansen, Maria Elisabeth; Ulven, Trond.

In: International Journal of Pharmaceutics, Vol. 452, No. 1-2, 2013, p. 276-282.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Hagesaether, E, Christiansen, E, Due-Hansen, ME & Ulven, T 2013, 'Mucus can change the permeation rank order of drug candidates', International Journal of Pharmaceutics, vol. 452, no. 1-2, pp. 276-282. https://doi.org/10.1016/j.ijpharm.2013.05.036

APA

Hagesaether, E., Christiansen, E., Due-Hansen, M. E., & Ulven, T. (2013). Mucus can change the permeation rank order of drug candidates. International Journal of Pharmaceutics, 452(1-2), 276-282. https://doi.org/10.1016/j.ijpharm.2013.05.036

Vancouver

Hagesaether E, Christiansen E, Due-Hansen ME, Ulven T. Mucus can change the permeation rank order of drug candidates. International Journal of Pharmaceutics. 2013;452(1-2):276-282. https://doi.org/10.1016/j.ijpharm.2013.05.036

Author

Hagesaether, Ellen ; Christiansen, Elisabeth ; Due-Hansen, Maria Elisabeth ; Ulven, Trond. / Mucus can change the permeation rank order of drug candidates. In: International Journal of Pharmaceutics. 2013 ; Vol. 452, No. 1-2. pp. 276-282.

Bibtex

@article{2aaf3bd6cc104065bbfbc9cf6033cf71,

title = "Mucus can change the permeation rank order of drug candidates",

abstract = "The aim of the study was to test the effect of mucus on the permeability of newly developed structurally related free fatty acid receptor 1-agonists TUG-488, TUG-499 and TUG-424, which were compared to the more hydrophilic ketoprofen and the more hydrophobic testosterone as reference drugs. The model membrane was cell monolayers consisting of methotrexate treated HT29 cells grown for approximately one, two or three weeks, and thereby differing in the amount of goblet cells and hence mucus. The results show that the permeation of all compounds was high and that mucus in most cases only had a minor influence. However, for one of the drug candidates, TUG-499, mucus had a clear impact, and this could not be explicitly related to the hydrophobicity of this compound. Secreted mucus thus changed the obtained rank order of permeation. This was especially apparent when the experiments were carried out at a lower agitation. These results indicate that an experimental system without mucus can give a faulty rank order of permeation compared to mucous membranes when structurally related drug candidates are tested.",

author = "Ellen Hagesaether and Elisabeth Christiansen and Due-Hansen, {Maria Elisabeth} and Trond Ulven",

year = "2013",

doi = "10.1016/j.ijpharm.2013.05.036",

language = "English",

volume = "452",

pages = "276--282",

journal = "International Journal of Pharmaceutics",

issn = "0378-5173",

publisher = "Elsevier",

number = "1-2",

}

RIS

TY - JOUR

T1 - Mucus can change the permeation rank order of drug candidates

AU - Hagesaether, Ellen

AU - Christiansen, Elisabeth

AU - Due-Hansen, Maria Elisabeth

AU - Ulven, Trond

PY - 2013

Y1 - 2013

N2 - The aim of the study was to test the effect of mucus on the permeability of newly developed structurally related free fatty acid receptor 1-agonists TUG-488, TUG-499 and TUG-424, which were compared to the more hydrophilic ketoprofen and the more hydrophobic testosterone as reference drugs. The model membrane was cell monolayers consisting of methotrexate treated HT29 cells grown for approximately one, two or three weeks, and thereby differing in the amount of goblet cells and hence mucus. The results show that the permeation of all compounds was high and that mucus in most cases only had a minor influence. However, for one of the drug candidates, TUG-499, mucus had a clear impact, and this could not be explicitly related to the hydrophobicity of this compound. Secreted mucus thus changed the obtained rank order of permeation. This was especially apparent when the experiments were carried out at a lower agitation. These results indicate that an experimental system without mucus can give a faulty rank order of permeation compared to mucous membranes when structurally related drug candidates are tested.

AB - The aim of the study was to test the effect of mucus on the permeability of newly developed structurally related free fatty acid receptor 1-agonists TUG-488, TUG-499 and TUG-424, which were compared to the more hydrophilic ketoprofen and the more hydrophobic testosterone as reference drugs. The model membrane was cell monolayers consisting of methotrexate treated HT29 cells grown for approximately one, two or three weeks, and thereby differing in the amount of goblet cells and hence mucus. The results show that the permeation of all compounds was high and that mucus in most cases only had a minor influence. However, for one of the drug candidates, TUG-499, mucus had a clear impact, and this could not be explicitly related to the hydrophobicity of this compound. Secreted mucus thus changed the obtained rank order of permeation. This was especially apparent when the experiments were carried out at a lower agitation. These results indicate that an experimental system without mucus can give a faulty rank order of permeation compared to mucous membranes when structurally related drug candidates are tested.

U2 - 10.1016/j.ijpharm.2013.05.036

DO - 10.1016/j.ijpharm.2013.05.036

M3 - Journal article

VL - 452

SP - 276

EP - 282

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -

ID: 189161777