ArticlePharmaceutical research2009
Synthesis, characterization and in vivo efficacy of PEGylated insulin for oral delivery with complexation hydrogels.
Article in Pharmaceutical research, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
5 citing papers in PubMed, 43 citations in OpenAlex.
- Development of Nanocarrier-Based Oral Pegfilgrastim Formulations for Mitigating Hematopoietic Acute Radiation Syndrome.Advanced functional materials · 2025Article
- Site-Selective Approaches to Attain Fluorescent Human Insulin Conjugates: Balancing the Site of Labeling and theACS omega · 2025Article
- Designing the new generation of intelligent biocompatible carriers for protein and peptide delivery.Acta pharmaceutica Sinica. B · 2018Review
- Article
- Approaches for enhancing oral bioavailability of peptides and proteins.International journal of pharmaceutics · 2013Review
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
purposeThis work evaluated the feasibility of combining insulin PEGylation with pH responsive hydrogels for oral insulin delivery.
methodsA mono-substituted PEG-insulin conjugate was synthesized and purified. The site of conjugation was determined by MALDI-TOF MS. Uptake and release of PEGylated insulin was performed in complexation hydrogels to simulate oral dosing. The bioactivity of the conjugate and PK/PD profile was measured in vivo in rats.
resultsPEGylation was confirmed to be specifically located at the amino terminus of the B-chain of insulin. Higher loading efficiency was achieved with PEGylated insulin than regular human insulin in pH responsive hydrogels. The release of PEGylated insulin was lower than that of human insulin at all pH levels considered. Full retention of bioactivity of the PEG-insulin conjugate was confirmed by intravenous dosing while subcutaneous dosing exhibited a relative hypoglycemic effect 127.8% that of human insulin.
conclusionsPolyethylene glycol conjugated specifically to the amino terminus of the B-chain of insulin maintained the bioactivity of the protein and significantly extended the duration of the hypoglycemic effect. Used in combination with pH responsive hydrogels, PEGylated insulin has significant potential for oral delivery.
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Registered trials
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