Evidence map›Paper›PMID 34100217›Full record

ArticlePharmaceutical research2021

Lipophilic Salts and Lipid-Based Formulations: Enhancing the Oral Delivery of Octreotide.

Peng Li, Leigh Ford, Shadabul Haque, Mitchell P McInerney, Hywel D Williams, Peter J Scammells, Philip E Thompson, Vincent Jannin, Christopher J H Porter, Hassan Benameur and 1 more

Abstract read
PubMed Publisher
In one paragraph

Article in Pharmaceutical research, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
0.9field-weighted citation impact, top 31% 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

7 citing papers in PubMed, 11 citations in OpenAlex.

  1. Article
  2. Review
  3. Review
  4. Article
  5. Article
  6. Acromegaly: Pathophysiological Considerations and Treatment Options Including the Evolving Role of Oral Somatostatin Analogs.Pathophysiology : the official journal of the International Society for Pathophysiology · 2023
    Review
  7. Article
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

11 authors at 1 institution in 1 country.

Peng LiOral Drug Delivery Innovation, Lonza Global R&D, Melbourne, Australia.
Leigh FordOral Drug Delivery Innovation, Lonza Global R&D, Melbourne, Australia.
Shadabul HaqueDrug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, Australia.
Mitchell P McInerneyCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, Australia.
Hywel D WilliamsOral Drug Delivery Innovation, Lonza Global R&D, Melbourne, Australia.
Peter J ScammellsMedicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, Australia.
Philip E ThompsonMedicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, Australia.
Vincent JanninOral Drug Delivery Innovation, Lonza Global R&D, Strasbourg, France.
Christopher J H PorterDrug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, Australia. chris.porter@monash.edu.
Hassan BenameurDrug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, Australia. hassan.benameur@monash.edu.
Colin W PoutonDrug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, Australia. colin.pouton@monash.edu.
Monash University · AU

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeSuccessful oral peptide delivery faces two major hurdles: low enzymatic stability in the gastro-intestinal lumen and poor intestinal membrane permeability. While lipid-based formulations (LBF) have the potential to overcome these barriers, effective formulation of peptides remains challenging. Lipophilic salt (LS) technology can increase the apparent lipophilicity of peptides, making them more suitable for LBF.

methodsAs a model therapeutic peptide, octreotide (OCT) was converted to the docusate LS (OCT.DoS

resultsLS formulation improved the solubility and loading of OCT in LBF excipients and OCT.DoS

conclusionThe combination of LS and LBF enhanced the in vivo oral absorption of OCT primarily via the protective effect of LBF sheltering the peptide from gastrointestinal degradation.

Indexed as

Administration, OralAnimalsCaco-2 CellsDrug CompoundingDrug Delivery SystemsExcipientsGastrointestinal AbsorptionGastrointestinal AgentsHumansMaleOctreotideRatsRats, Sprague-DawleySaltsExcipientsGastrointestinal AgentsOctreotideSaltslipid-based formulationslipophilic saltsoctreotideoral deliverypeptides

Identifiers

PMID34100217
OpenAlexW3167094908

What OpenQuestion holds

Textmetadata
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.