Aqueous remote loading of setmelanotide in poly(lactic-co-glycolic acid) microspheres for long-term obesity treatment.

Wang S, Downing G, Olsen KF, Sawyer TK, Cone RD, Schwendeman SP

Journal of controlled release : official journal of the Controlled Release Society15 Nov 2023Cited by 12 (Europe PMC)

PMID37678438DOI10.1016/j.jconrel.2023.09.015PepBankPUB-37678438

Publisher page PubMedAsk about this study

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

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

01AnimalAnimal study (in vivo)Pharmacokinetics
In obese mice, setmelanotide-loaded microspheres showed less initial burst and slightly faster overall release than the in vitro profile.
In plain wordsIn mice, setmelanotide-loaded microspheres released less peptide initially but released it faster overall than in lab tests.
Peptide
Setmelanotide
Outcome
MixedIn vivo release profile
Study
mousen: not reported in source
diet-induced obese murine model
Comparator
in vitro release profile
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · subcutaneousAs given in this study (mouse).
Source sentences
Summary
The obtained in vivo release pattern from deconvolution of the pharmacokinetics after subcutaneous microsphere injection was consistent with the in vitro release profile but with a lower initial burst release and overall slightly faster release rate.
1 context sentence(design, population, supporting numbers)
Summary · context
A diet-induced obese murine model was then used to determine the pharmacokinetic profile and to evaluate long-term efficacy of an optimal formulation.
Report a problemFND-3767843804
02AnimalAnimal study (in vivo)Efficacy outcome
In obese mice, one injection of setmelanotide-loaded PLGA microspheres inhibited food intake over 17 days.
In plain wordsIn obese mice, one injection of setmelanotide-loaded PLGA microspheres suppressed food intake over 17 days.
Peptide
Setmelanotide
Outcome
DecreaseFood intake
Study
mousen: not reported in source
diet-induced obese murine model
Outcome group
Appetite and food intake · Metabolic and weight
Studied dose
Dose not stated · subcutaneousAs given in this study (mouse).
Source sentences
Summary
After a single injection of remote-loaded setmelanotide, continuous long-term inhibition of food intake and body weight control was observed over 17 and 30 days, respectively.
2 context sentences(design, population, supporting numbers)
Summary · context
A diet-induced obese murine model was then used to determine the pharmacokinetic profile and to evaluate long-term efficacy of an optimal formulation.
Summary · context
The obtained in vivo release pattern from deconvolution of the pharmacokinetics after subcutaneous microsphere injection was consistent with the in vitro release profile but with a lower initial burst release and overall slightly faster release rate.
Report a problemFND-3767843805
03AnimalAnimal study (in vivo)Efficacy outcome
In obese mice, setmelanotide-loaded PLGA microspheres improved body weight control over 30 days versus drug-free microspheres.
In plain wordsIn obese mice, setmelanotide-loaded PLGA microspheres improved weight control over 30 days compared with drug-free microspheres.
Peptide
Setmelanotide
Outcome
DecreaseBody weight control
Study
mousen: not reported in source
diet-induced obese murine model
Comparator
drug-free microsphere vehicle
Outcome group
Body weight · Metabolic and weight
Studied dose
Dose not stated · subcutaneousAs given in this study (mouse).
Source sentences
Summary
After a single injection of remote-loaded setmelanotide, continuous long-term inhibition of food intake and body weight control was observed over 17 and 30 days, respectively.
3 context sentences(design, population, supporting numbers)
Summary · context
The improvement in body weight control over drug-free microsphere vehicle-treated control groups matched the observed PK profile.
Summary · context
A diet-induced obese murine model was then used to determine the pharmacokinetic profile and to evaluate long-term efficacy of an optimal formulation.
Summary · context
The obtained in vivo release pattern from deconvolution of the pharmacokinetics after subcutaneous microsphere injection was consistent with the in vitro release profile but with a lower initial burst release and overall slightly faster release rate.
Report a problemFND-3767843806

Studies that did not test the peptide alone3

In this study, Setmelanotide 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 Setmelanotide.

04LabNot a test of Setmelanotide aloneIn vitro (cell-free)Other
In lab tests, increased PLGA microsphere density inhibited setmelanotide encapsulation.
In plain wordsIn lab tests, denser PLGA microspheres reduced setmelanotide encapsulation.
Peptide
Setmelanotide
Outcome
DecreaseEncapsulation and density
Study
n: not reported in source
PLGA microspheres
Outcome group
Drug Formulation · Pharmacology
Source sentences
Summary
Increased density of the microspheres inhibited the progress of encapsulation of the dicationic peptide.
1 context sentence(design, population, supporting numbers)
Summary · context
Here we sought to remote-load setmelanotide in PLGA microspheres and examine its potential for long-term controlled release and body weight control.
In this study, Setmelanotide 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 Setmelanotide.
Report a problemFND-3767843801
05LabNot a test of Setmelanotide aloneIn vitro (cell-free)Other
In lab tests, PLGA microspheres encapsulated setmelanotide at up to ∼63%, with ∼6.3% w/w loading.
In plain wordsIn lab tests, PLGA microspheres encapsulated setmelanotide at up to ∼63%.
Peptide
Setmelanotide
Outcome
Not applicableDrug encapsulation
Study
n: not reported in source
PLGA microspheres
Outcome group
Drug Formulation · Pharmacology
Source sentences
Summary
Remote loaded PLGA formulations encapsulated setmelanotide as high as ∼63% (∼6.3% w/w loading) and exhibited slow and continuous peptide release over ∼6 weeks in vitro largely independent of microsphere porosity.
1 context sentence(design, population, supporting numbers)
Summary · context
Here we sought to remote-load setmelanotide in PLGA microspheres and examine its potential for long-term controlled release and body weight control.
In this study, Setmelanotide 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 Setmelanotide.
Report a problemFND-3767843802
06LabNot a test of Setmelanotide aloneIn vitro (cell-free)Pharmacokinetics
In lab tests, setmelanotide-loaded PLGA microspheres released peptide slowly and continuously over ∼6 weeks, largely independently of porosity.
In plain wordsIn lab tests, setmelanotide-loaded PLGA microspheres released peptide slowly over ∼6 weeks, largely independently of porosity.
Peptide
Setmelanotide
Outcome
Not applicableIn vitro release
Study
n: not reported in source
PLGA microspheres
Outcome group
Pharmacokinetics · Pharmacology
Source sentences
Summary
Remote loaded PLGA formulations encapsulated setmelanotide as high as ∼63% (∼6.3% w/w loading) and exhibited slow and continuous peptide release over ∼6 weeks in vitro largely independent of microsphere porosity.
1 context sentence(design, population, supporting numbers)
Summary · context
Here we sought to remote-load setmelanotide in PLGA microspheres and examine its potential for long-term controlled release and body weight control.
In this study, Setmelanotide 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 Setmelanotide.
Report a problemFND-3767843803

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
28 Oct 2026, 02:03 UTC
Study results updated
Version 1
27 Oct 2026, 16:36 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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