Mucopenetrating micelles with a PEG coronaElectronic supplementary information (ESI) available: NMR spectra, emission spectra for CMC assessment, TEM images of cargo-loaded micelles, basic characterization of Caco-2/HT29-MTX-E12 co-cultures, and supporting experiment for mucopenetration in cell culture. See DOI: 10.1039/c7nr06821b

• Main Authors: Taipaleenmäki, Essi M, Mouritzen, Sidsel A, Schattling, Philipp S, Zhang, Yan, Städler, Brigitte
• Format: Article
• Language: English
• ISSN: 2040-3364; 2040-3372
• DOI: 10.1039/c7nr06821b

Crossing the intestinal mucus layer is a long-standing challenge for orally delivered nanoparticles carrying therapeutic cargo. We report the assembly of mucopenetrating cargo-loaded micelles using block copolymers consisting of either linear poly(ethylene glycol) (PEG) or bottle-brush poly(oligo(ethylene glycol)methacrylate) (PEG b ) as the hydrophilic block and poly(caprolactone) (PCL) or poly(cholesteryl methacrylate) (PCMA) as the hydrophobic extension. The micelles were shown to preserve their stability and retain ∼50% of their cargo in simulated gastric fluid. The ability of micelles to diffuse through reconstituted porcine mucus was assessed in a microfluidic set-up. Finally, the delivery of Nile Red as a hydrophobic model cargo across a mucus layer produced by epithelial cells was demonstrated. These engineered mucopenetrating micelles have potential to be developed into efficient absorption enhancers, contributing a nanotechnology solution to oral drug delivery. The mucopenetrating properties of cargo-loaded micelles with a PEG corona are characterized in a microfluidic set-up and in cell culture.