In vivo evaluation of an oral self-emulsifying drug delivery system (SEDDS) for exenatide.

Menzel C, Holzeisen T, Laffleur F, Zaichik S, Abdulkarim M, Gumbleton M, Bernkop-Schnürch A

Journal of controlled release : official journal of the Controlled Release Society21 Mar 2018Cited by 94 (Europe PMC)

PMID29574041DOI10.1016/j.jconrel.2018.03.018PepBankPUB-29574041

Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study6

2 results from studies that gave the peptide. No result from this study comes from people.

01AnimalAnimal study (in vivo)Pharmacokinetics
In healthy male rats, oral exenatide/DOC SEDDS had relative bioavailability of 14.62% ± 3.07% versus subcutaneous administration.
In plain wordsIn rats, oral formulated exenatide had measured availability relative to an injection under the skin.
Peptide
Exenatide (exendin-4)
Outcome
Not applicableRelative oral bioavailability
Study
ratn: not reported in source
healthy male Sprague-Dawley rats
Comparator
Subcutaneous exenatide
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · oralAs given in this study (rat).
Source sentences
Summary
Orally administered exenatide/DOC SEDDS showed a relative bioavailability (versus s.c.) of 14.62% ± 3.07% and caused a significant (p < .05) 20.6% decrease in AUC values of blood glucose levels.
1 context sentence(design, population, supporting numbers)
Summary · context
Furthermore, the impact of orally administered exenatide/DOC SEDDS on blood glucose level was investigated in vivo on healthy male Sprague-Dawley rats.
Report a problemFND-2957404105
02AnimalAnimal study (in vivo)Efficacy outcome
In healthy male rats, oral exenatide/DOC SEDDS significantly decreased blood glucose AUC by 20.6%.
In plain wordsIn rats, oral formulated exenatide reduced overall blood sugar exposure.
Peptide
Exenatide (exendin-4)
Outcome
DecreaseBlood glucose AUC
Study
ratn: not reported in source
healthy male Sprague-Dawley rats
Outcome group
Glycemic control · Metabolic and weight
Studied dose
Dose not stated · oralAs given in this study (rat).
Source sentences
Summary
Orally administered exenatide/DOC SEDDS showed a relative bioavailability (versus s.c.) of 14.62% ± 3.07% and caused a significant (p < .05) 20.6% decrease in AUC values of blood glucose levels.
1 context sentence(design, population, supporting numbers)
Summary · context
Furthermore, the impact of orally administered exenatide/DOC SEDDS on blood glucose level was investigated in vivo on healthy male Sprague-Dawley rats.
Report a problemFND-2957404106

Studies that did not test the peptide alone4

In this study, Exenatide (exendin-4) was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Exenatide (exendin-4).

03LabNot a test of Exenatide (exendin-4) aloneIn vitro (cell-free)Activity measurement
In laboratory tests, ion pairing exenatide with DOC increased effective logP from -1.1 to 2.1.
In plain wordsIn lab tests, pairing exenatide with DOC increased its lipid affinity compared with unpaired exenatide.
Peptide
Exenatide (exendin-4)
Outcome
IncreaseEffective logP
Study
n: not reported in source
Comparator
Exenatide before ion pairing
Outcome group
Formulation, delivery and stability · Pharmacology
Source sentences
Summary
Hydrophobic ion pairing in a molar ratio of 1:4 (exenatide:DOC) increased the effective logP of exenatide from -1.1 to 2.1.
In this study, Exenatide (exendin-4) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Exenatide (exendin-4).
Report a problemFND-2957404101
04LabNot a test of Exenatide (exendin-4) aloneIn vitro (cell-free)Activity measurement
In laboratory tests, exenatide/DOC SEDDS had a mean droplet size of 45.87 ± 2.9 nm.
In plain wordsIn lab tests, the exenatide formulation formed droplets with a measured average size.
Peptide
Exenatide (exendin-4)
Outcome
Not applicableDroplet size
Study
n: not reported in source
Outcome group
Formulation, delivery and stability · Pharmacology
Source sentences
Summary
SEDDS with a payload of 1% exenatide/DOC had a mean droplet size of 45.87 ± 2.9 nm and a Log D_{SEDDS/release medium} of 1.9 ± 0.05.
In this study, Exenatide (exendin-4) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Exenatide (exendin-4).
Report a problemFND-2957404102
05LabNot a test of Exenatide (exendin-4) aloneIn vitro (cell-free)Activity measurement
In laboratory tests, exenatide/DOC SEDDS had a release-medium Log D of 1.9 ± 0.05.
In plain wordsIn lab tests, researchers measured how exenatide distributed between its formulation and release liquid.
Peptide
Exenatide (exendin-4)
Outcome
Not applicableSEDDS release partition coefficient
Study
n: not reported in source
Outcome group
Formulation, delivery and stability · Pharmacology
Source sentences
Summary
SEDDS with a payload of 1% exenatide/DOC had a mean droplet size of 45.87 ± 2.9 nm and a Log D_{SEDDS/release medium} of 1.9 ± 0.05.
In this study, Exenatide (exendin-4) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Exenatide (exendin-4).
Report a problemFND-2957404103
06LabNot a test of Exenatide (exendin-4) aloneIn vitro (cell-free)Activity measurement
In laboratory permeation tests, exenatide/DOC SEDDS improved mucus diffusion 2.7-fold versus exenatide in solution.
In plain wordsIn lab tests, formulated exenatide moved through mucus more readily than exenatide in solution.
Peptide
Exenatide (exendin-4)
Outcome
IncreaseMucus diffusion
Study
n: not reported in source
Comparator
Exenatide in solution
Outcome group
Pharmacokinetics · Pharmacology
Source sentences
Summary
Permeation experiments revealed 2.7-fold improved mucus diffusion for exenatide/DOC SEDDS compared to exenatide in solution.
In this study, Exenatide (exendin-4) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Exenatide (exendin-4).
Report a problemFND-2957404104

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
22 Oct 2026, 02:26 UTC
Study results updated
Version 1
21 Oct 2026, 18:59 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

Publication types

Journal Article

MeSH terms

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