ArticleScientific reports2023
Mercaptonicotinic acid activated thiolated chitosan (MNA-TG-chitosan) to enable peptide oral delivery by opening cell tight junctions and enhancing transepithelial transport.
Article in Scientific reports, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 15 citations in OpenAlex.
- Article
- Food-derived molecules as regulators of intestinal tight junctions and barrier function: mechanisms and implications.Frontiers in drug delivery · 2026Review
- The concurrent silencing of Tim-3 and STAT-3 promotes tumor regression both in vitro and in ovo.BMC cancer · 2025Article
- The Transformative Role of Nanotechnology in the Management of Diabetes Mellitus: Insights from Current Research.Biomolecules · 2025Review
- Topical Ocular Drug Delivery: The Impact of Permeation Enhancers.Pharmaceutics · 2025Review
- Transmucosal Delivery of miR-30c-5p by Chitosan Nanoparticles for Oral Squamous Cell Carcinoma.International journal of nanomedicine · 2025Article
- Advancements in insulin delivery: the potential of natural polymers for improved diabetes management.Frontiers in bioengineering and biotechnology · 2025Review
- Advances in Nanomedicine for Precision Insulin Delivery.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Nanostructure-Mediated Transport of Therapeutics through Epithelial Barriers.International journal of molecular sciences · 2024Review
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Recent advances in peptide delivery and nanotechnology has resulted in emergence of several non-parenteral administration routes that replace subcutaneous injections associated with patient discomfort. Thiolated biopolymers are relatively new materials being explored to enhance mucoadhesivity and permeability in these efforts, yet their pH dependent reactivity remains an obstacle. This work focussed on improving the mucoadhesivity of thiolated chitosans by activating them with mercaptonicotinic acid, in a bid to create a novel thiomerized chitosan that can open cell tight junctions for application in oral delivery. The synthesized mercaptonicotinic acid activated thiolated chistoan (MNA-TG-chitosan), along with thiolated chitosan (TG-chitosan) and unmodified chitosan were then used to create insulin nanoparticles (insNPs) using spray drying encapsulation process. Use of MNA-TG-chitosan in place of chitosan resulted in reduction of particle size of insNPs from 318 to 277 nm with no significant changes in polydispersity index (~ 0.2), encapsulation efficiency (~ 99%), insulin loading content (~ 25%) and morphology. Results from in-vitro cytotoxicity on TR146, CaCo2 and HepG2 cell lines revealed no significant effects on cell viability at 50-1000 μg/mL concentration. insNPs encapsulated with the new material, MNA-TG-chitosan, resulted in a 1.5-fold and 4.4-fold higher cellular uptake by HepG2 liver cells where insulin is metabolized, approximately 40% and 600% greater insulin transport through TR146 buccal cell monolayers, and 40% and 150% greater apparent permeability than insNPs encapsulated with unmodified chitosan and TG-chitosan respectively. The higher permeation achieved on using MNA-TG chitosan was attributed to the greater opening of the cell tight junction evidenced by reduction of transepithelial electrical resistance of TR146 buccal cell monolayers. This study demonstrates MNA-TG-chitosan as a promising material for improved peptide oral delivery.
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