Universität zu Köln

Classen, Rebecca, Pouokam, Ervice, Wickleder, Matthias, Diener, Martin and Mattern, Annabelle (2022). Atropine-functionalized gold nanoparticles binding to muscarinic receptors after passage across the intestinal epithelium. R. Soc. Open Sci., 9 (10). LONDON: ROYAL SOC. ISSN 2054-5703

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Abstract

Gold nanoparticles have a high potential to be a treatment of diseases by their specific drug delivery properties and multivalent receptor stimulation. For the present project, spherical gold nanoparticles were synthesized and functionalized with the muscarinic receptor antagonist atropine (Au-MUDA-AT NPs). The diameter of the gold core could precisely be controlled by using different synthetic methods and reducing agents resulting in functionalized gold nanoparticles with diameters ranging from 8 to 16 nm. The ability to interact with intestinal muscarinic receptors is size-dependent. When using intestinal chloride secretion induced by the stable acetylcholine derivative, carbachol, as read-out, the strongest inhibition, i.e. the most efficient blockade of muscarinic receptors, was observed with 13 nm sized Au-MUDA-AT NPs. Functional experiments indicate that Au-MUDA-AT NPs with a diameter of 14 nm are able to pass the intestinal mucosa in a time-dependent manner after administration to the intestinal lumen. For example, luminally administered Au-MUDA-AT NPs inhibited contractions of the small intestinal longitudinal muscle layer induced by electrical stimulation of myenteric neurons. A similar inhibition of basolateral epithelial receptors was observed after luminal administration of Au-MUDA-AT NPs when using carbachol-induced chloride secretion across the intestinal epithelium as a test system. Thus, Au-MUDA-AT NPs might be a therapeutic tool for the modulation of intestinal secretion and motility after oral application in the future.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Classen, Rebecca UNSPECIFIED UNSPECIFIED UNSPECIFIED Pouokam, Ervice UNSPECIFIED UNSPECIFIED UNSPECIFIED Wickleder, Matthias UNSPECIFIED UNSPECIFIED UNSPECIFIED Diener, Martin UNSPECIFIED UNSPECIFIED UNSPECIFIED Mattern, Annabelle UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-669870
DOI:	10.1098/rsos.220244
Journal or Publication Title:	R. Soc. Open Sci.
Volume:	9
Number:	10
Date:	2022
Publisher:	ROYAL SOC
Place of Publication:	LONDON
ISSN:	2054-5703
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language RAT COLON; SIZE; SECRETION; SHAPE Multiple languages Multidisciplinary Sciences Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/66987