Evidence map›Paper›PMID 38544951›Full record

ArticleInternational journal of nanomedicine2024

Coordinated ASBT and EGFR Mechanisms for Optimized Liraglutide Nanoformulation Absorption in the GI Tract.

Seho Kweon, Seong Jin Park, Ha Kyeong Lee, Seo Hee Kang, Kwan-Young Chang, Jeong Uk Choi, Jooho Park, Jung-Hyun Shim, Jin Woo Park, Youngro Byun

Open access · goldAbstract read
In one paragraph

Article in International journal of nanomedicine, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed, 1 pooled it
4.7field-weighted citation impact, top 5% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

The trial behind it

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

5 citing papers in PubMed, 1 synthesis or guideline pooled it, 13 citations in OpenAlex.

  1. Pooled it
  2. Review
  3. Article
  4. Review
  5. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 5 institutions in 1 country.

Seho KweonDepartment of Molecular Medicine and Biopharmaceutical Science, Graduate School of Convergence Science and Technology, Seoul National University, Seoul, 08826, Republic of Korea.
Seong Jin ParkCollege of Pharmacy, Seoul National University, Seoul, 08826, Republic of Korea.
Ha Kyeong LeeDepartment of Molecular Medicine and Biopharmaceutical Science, Graduate School of Convergence Science and Technology, Seoul National University, Seoul, 08826, Republic of Korea.
Seo Hee KangGlobal R&D Center, IcureBNP, Seoul, 06170, Republic of Korea.
Kwan-Young ChangGlobal R&D Center, IcureBNP, Seoul, 06170, Republic of Korea.
Jeong Uk ChoiCollege of Pharmacy, Kyung Hee University, Seoul, 02447, Republic of Korea.
Jooho ParkDepartment of Biomedical & Health Science, Konkuk University, Chungju, 27478, Republic of Korea.ORCID 0000-0001-6332-3278
Jung-Hyun ShimCollege of Pharmacy and Biomedical and Healthcare Research Institute, Mokpo National University, Jeonnam, 58554, Republic of Korea.ORCID 0000-0002-4062-4016
Jin Woo ParkCollege of Pharmacy and Biomedical and Healthcare Research Institute, Mokpo National University, Jeonnam, 58554, Republic of Korea.ORCID 0000-0002-0001-7043
Youngro ByunDepartment of Molecular Medicine and Biopharmaceutical Science, Graduate School of Convergence Science and Technology, Seoul National University, Seoul, 08826, Republic of Korea.
Mokpo National University · KRSeoul National University · KRKorea Pharma (South Korea) · KRChonnam National University · KRKyung Hee University · KR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Background: For maintenance therapy in type 2 diabetes, glucagon-like peptide-1 agonist (GLP-1A), which exhibits low cardiovascular risk and high efficacy, is a promising peptide therapeutic. However, developing an oral GLP-1A presents challenges due to the analog's poor cellular permeability and gastrointestinal (GI) stability. Methods: To mitigate such limitations, an oral nanoformulation of liraglutide (LG) was designed and achieved by combining LG with bile acid derivatives using the nanoprecipitation method. This strategy allowed the bile acid moieties to localize at the nanoparticle surface, enhancing the binding affinity for apical sodium-dependent bile acid transporter (ASBT) and improving GI stability. The in vitro characteristics, cellular permeability, and absorption mechanisms of the LG nanoformulation (LG/TD-NF) were thoroughly investigated. Furthermore, the in vivo oral absorption in rats and the glucose-lowering effects in a diabetic ( Results: The LG/TD-NF produced neutral nanoparticles with a diameter of 58.7 ± 4.3 nm and a zeta potential of 4.9 ± 0.4 mV. Notably, when exposed to simulated gastric fluid, 65.7 ± 3.6% of the LG/TD-NF remained stable over 120 min, while free LG was fully degraded. Relative to unformulated LG, the Caco-2 cellular permeability of the nanoformulation improved, measuring 10.9 ± 2.1 (× 10 Conclusion: The oral LG/TD-NF promotes ASBT/EGFR-mediated transcytosis and assures cellular permeability within the GI tract. This method holds promise for the development of oral GLP-1A peptides as an alternative to injections, potentially enhancing patient adherence to maintenance therapy.

Indexed as

Diabetes Mellitus, Type 2LiraglutideAnimalsBile Acids and SaltsCaco-2 CellsErbB ReceptorsGastrointestinal TractGlucagon-Like Peptide 1GlucoseHumansHypoglycemic AgentsMiceRatsBile Acids and SaltsEGFR protein, humanErbB ReceptorsGlucagon-Like Peptide 1GlucoseHypoglycemic AgentsLiraglutideASBT-mediated endocytosisEGFRnanoformulation of GLP-1Aoral liraglutide

Identifiers

PMID38544951
PMCPMC10968941
OpenAlexW4393119943

What OpenQuestion holds

Texttitle and abstract
LicenceCC BY-NC
Read underepoch 390

Registered trials

None linked

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.