ArticlePharmaceutical research2011
Uptake and transport of novel amphiphilic polyelectrolyte-insulin nanocomplexes by Caco-2 cells--towards oral insulin.
Article in Pharmaceutical research, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 52 citations in OpenAlex.
- Challenges and Opportunities in the Oral Delivery of Recombinant Biologics.Pharmaceutics · 2023Review
- Nanoparticle Delivery Systems in the Treatment of Diabetes Complications.Molecules (Basel, Switzerland) · 2019Review
- A Novel PAA Derivative with Enhanced Drug Efficacy in Pancreatic Cancer Cell Lines.Pharmaceuticals (Basel, Switzerland) · 2018Article
- Pre-formulation and systematic evaluation of amino acid assisted permeability of insulin across in vitro buccal cell layers.Scientific reports · 2016Article
- Developments in Methods for Measuring the Intestinal Absorption of Nanoparticle-Bound Drugs.International journal of molecular sciences · 2016Review
- Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects.Pharmaceutical research · 2016Article
- Permeation of insulin, calcitonin and exenatide across Caco-2 monolayers: measurement using a rapid, 3-day system.PloS one · 2013Article
- The use of nano polymeric self-assemblies based on novel amphiphilic polymers for oral hydrophobic drug delivery.Pharmaceutical research · 2012Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe influence of polymer architecture on cellular uptake and transport across Caco-2 cells of novel amphiphilic polyelectrolyte-insulin nanocomplexes was investigated.
methodPolyallylamine (PAA) (15 kDa) was grafted with palmitoyl chains (Pa) and subsequently modified with quaternary ammonium moieties (QPa). These two amphiphilic polyelectrolytes (APs) were tagged with rhodamine, and their uptake by Caco-2 cells or their polyelectrolyte complexes (PECs) with fluorescein isothiocyanate-insulin (FITC-insulin) uptake was investigated using fluorescence microscopy. The integrity of the monolayer was determined by measurement of transepithelial electrical resistance (TEER), and insulin transport across the monolayers was determined.
resultPa and insulin were co-localised in cell membranes, while QPa complexes were found within the cytoplasm. QPa complex uptake was not affected by calcium, cytochalasin D or nocodazole. Uptake was reduced by co-incubation with sodium azide, an active transport inhibitor. Both polymers opened tight junctions reversibly, and insulin transport through monolayers increased when QPa or Pa was used.
conclusionThese APs have been shown to be taken up by Caco-2 cells and reversibly open tight cell junctions. Further work is required to optimise these formulations with a view to maximising their potential to facilitate oral delivery of insulin.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.