ArticlePharmaceutical research2014
Acylation of exenatide by glycolic acid and its anti-diabetic activities in db/db mice.
Article in Pharmaceutical research, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 14 citations in OpenAlex.
- Peptide Acylation in Aliphatic Polyesters: a Review of Mechanisms and Inhibition Strategies.Pharmaceutical research · 2024Review
- Injectable sustained-release poly(lactic-co-glycolic acid) (PLGA) microspheres of exenatide prepared by supercritical fluid extraction of emulsion process based on a design of experiment approach.Bioengineering & translational medicine · 2023Article
- Recent Progress in Drug Release Testing Methods of Biopolymeric Particulate System.Pharmaceutics · 2021Review
- Effect of Stabilizers on Encapsulation Efficiency and Release Behavior of Exenatide-Loaded PLGA Microsphere Prepared by the W/O/W Solvent Evaporation Method.Pharmaceutics · 2019Article
- Comparison of ELISA and HPLC-MS methods for the determination of exenatide in biological and biotechnology-based formulation matrices.Journal of pharmaceutical analysis · 2019Review
- The extracellular domain of Staphylococcus aureus LtaS binds insulin and induces insulin resistance during infection.Nature microbiology · 2018Article
- Sustained-release study on Exenatide loaded into mesoporous silica nanoparticles: in vitro characterization and in vivo evaluation.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2017Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo prepare acylated exenatide analogues and investigate their biological properties for guiding the development of PLGA formulations of exenatide.
methodsThe acylated exenatide analogues were prepared by reaction with glycolic acid (GA), one constitutional unit of PLGA, and characterized by HPLC-MS/MS and Circular Dichroism (CD). The pharmacokinetic properties and anti-diabetic activities were studied in SD rats and db/db mice, respectively.
resultsStructural characterizations of the acylated products showed that one to four glycolic acids (GAs) were connected to the primary amine groups of exenatide, and there was a conversion of α-helix to β-sheet to some extent. Pharmacokinetic studies in SD rats revealed that acylated exenatides had a similar Tmax with that of the prototype drug, whereas the Cmax and the AUC values of the adducts were significantly decreased. Biological activity tests demonstrated that exenatide and acylated exenatide analogues had similar in vivo antidiabetic activities in terms of controlling blood glucose concentration, HbA1c level, body weight and food intake.
conclusionsThese findings suggest that GA conjugated exenatide had no influence on the peptide efficacy, therefore it's not necessary to inhibit exenatide acylation in PLGA formulations during the peptide release process.
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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.