ArticleInternational journal of nanomedicine2012
A silica-based pH-sensitive nanomatrix system improves the oral absorption and efficacy of incretin hormone glucagon-like peptide-1.
Article in International journal of nanomedicine, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
7 citing papers in PubMed, 1 synthesis or guideline pooled it, 23 citations in OpenAlex.
- Design strategies for chemical-stimuli-responsive programmable nanotherapeutics.Drug discovery today · 2019Pooled it
- Oral Treatment of Obesity by GLP-1 and Its Analogs.Pharmaceutics · 2025Review
- Peptide-Mediated Nanocarriers for Targeted Drug Delivery: Developments and Strategies.Pharmaceutics · 2024Review
- Improved systemic half-life of glucagon-like peptide-1-loaded carbonate apatite nanoparticles in rats.World journal of diabetes · 2022Article
- Nanodelivery systems and stabilized solid-drug nanoparticles for orally administered medicine: current landscape.International journal of nanomedicine · 2018Review
- pH-Responsive carriers for oral drug delivery: challenges and opportunities of current platforms.Drug delivery · 2017Review
- Stimuli-responsive nanocarriers for drug delivery.Nature materials · 2013Review
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundGlucagon-like peptide-1 (GLP-1) (7-36) is a peptide incretin hormone released from the endocrine L-cells of the intestinal mucosa with unique antidiabetic potential. Due to low absorption efficiency and instability in the gastrointestinal tract, the introduction of orally active GLP-1 is a large challenge. Here we developed a novel silica-based pH-sensitive nanomatrix of GLP-1 (SPN-GLP-1) in order to provide a strategy for oral peptide delivery.
methodsSPN-GLP-1 composed of silica nanoparticles and pH-sensitive Eudragit(®) was prepared and characterized by dynamic light scattering, scanning electron microscope, transmission electron microscope, high-performance liquid chromatography, surface analysis, drug release, and so on. Its permeability across the Caco-2 cell monolayer and intestinal mucosa, proteolytic stability against the intestinal enzymes, pharmacokinetics, hypoglycemic effect in the intraperitoneal glucose tolerance test (IPGTT), and primary toxicity were then evaluated.
resultsIt was indicated that the nanomatrix system obtained had a unique nanoscale structure and pH-sensitivity in drug release. It displayed a five-fold intestinal mucosa permeability and significantly higher proteolytic stability compared to native GLP-1 (P < 0.001). A longer half-life was observed after oral administration of SPN-GLP-1, and its relative bioavailability was 35.67% in comparison to intraperitoneal GLP-1. Oral delivery of SPN-GLP-1 significantly reduced the blood glucose level and its hypoglycemic effect over intraperitoneal GLP-1 reached 77%. There was no evident toxicity of SPN-GLP-1 found from both animal status and histochemical analysis of gastrointestinal tissues.
conclusionThe silica-based pH-sensitive nanomatrix designed and prepared here might be considered as a potential oral delivery system not only for GLP-1, but also for other peptide or macromolecular drugs.
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