Atropine-functionalized gold nanoparticles binding to muscarinic receptors after passage across the intestinal epithelium

Atropine-functionalized gold nanoparticles binding to muscarinic receptors after passage across the intestinal epithelium

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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 read more 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 Baby Tee 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.