Influence of Bile Composition on Membrane Incorporation of Transient Permeability Enhancers.


Journal

Molecular pharmaceutics
ISSN: 1543-8392
Titre abrégé: Mol Pharm
Pays: United States
ID NLM: 101197791

Informations de publication

Date de publication:
02 11 2020
Historique:
pubmed: 23 9 2020
medline: 15 9 2021
entrez: 22 9 2020
Statut: ppublish

Résumé

Transient permeability enhancers (PEs), such as caprylate, caprate, and salcaprozate sodium (SNAC), improve the bioavailability of poorly permeable macromolecular drugs. However, the effects are variable across individuals and classes of macromolecular drugs and biologics. Here, we examined the influence of bile compositions on the ability of membrane incorporation of three transient PEs-caprylate, caprate, and SNAC-using coarse-grained molecular dynamics (CG-MD). The availability of free PE monomers, which are important near the absorption site, to become incorporated into the membrane was higher in fasted-state fluids than that in fed-state fluids. The simulations also showed that transmembrane perturbation,

Identifiants

pubmed: 32960068
doi: 10.1021/acs.molpharmaceut.0c00668
pmc: PMC7610231
doi:

Substances chimiques

Bile Acids and Salts 0
Caprylates 0
Decanoates 0
Macromolecular Substances 0
N-(8-(2-hydroxybenzoyl)amino)caprylate 0
Phospholipids 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

4226-4240

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Auteurs

Shakhawath Hossain (S)

Department of Pharmacy, Uppsala University, Husargatan 3, 751 23 Uppsala, Sweden.
The Swedish Drug Delivery Forum (SDDF), Uppsala University, Husargatan 3, 751 23 Uppsala, Sweden.

Paul Joyce (P)

Division of Biological Physics, Chalmers University of Technology, 412 96 Gothenburg, Sweden.

Albin Parrow (A)

Department of Pharmacy, Uppsala University, Husargatan 3, 751 23 Uppsala, Sweden.

Silver Jõemetsa (S)

Division of Biological Physics, Chalmers University of Technology, 412 96 Gothenburg, Sweden.

Fredrik Höök (F)

Division of Biological Physics, Chalmers University of Technology, 412 96 Gothenburg, Sweden.

Per Larsson (P)

Department of Pharmacy, Uppsala University, Husargatan 3, 751 23 Uppsala, Sweden.
The Swedish Drug Delivery Forum (SDDF), Uppsala University, Husargatan 3, 751 23 Uppsala, Sweden.

Christel A S Bergström (CAS)

Department of Pharmacy, Uppsala University, Husargatan 3, 751 23 Uppsala, Sweden.
The Swedish Drug Delivery Forum (SDDF), Uppsala University, Husargatan 3, 751 23 Uppsala, Sweden.

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Classifications MeSH