Biodegradable PLGA microparticles for sustained release of a new GnRH antagonist: part II. In vivo performance.

Schwach G, Oudry N, Giliberto JP, Broqua P, Lück M, Lindner H, Gurny R

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V1 May 2004Cited by 13 (Europe PMC)

PMID15093591DOI10.1016/j.ejpb.2004.01.005PepBankPUB-15093591

Publisher page PubMedAsk about this study

Jump to 13 results

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 study13

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

01AnimalAnimal study (in vivo)Efficacy outcome
In castrated male rats, increasing degarelix microparticle dose accelerated onset of LH inhibition.
In plain wordsIn rats, increasing degarelix microparticle dose accelerated onset of LH inhibition.
Peptide
Degarelix
Outcome
DecreaseOnset of LH inhibition with increasing dose
Study
ratn: not reported in source
castrated male rat
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
0.4, 1.0 and 1.5 mg/kgAs given in this study (rat).
Source sentences
Summary
When increasing the dose, onset of inhibition was faster, inhibition was more intense, and duration of action was prolonged.
2 context sentences(design, population, supporting numbers)
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
Report a problemFND-1509359101
02AnimalAnimal study (in vivo)Efficacy outcome
In castrated male rats, increasing degarelix microparticle dose intensified LH inhibition.
In plain wordsIn rats, increasing degarelix microparticle dose intensified LH inhibition.
Peptide
Degarelix
Outcome
IncreaseIntensity of LH inhibition with increasing dose
Study
ratn: not reported in source
castrated male rat
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
0.4, 1.0 and 1.5 mg/kgAs given in this study (rat).
Source sentences
Summary
When increasing the dose, onset of inhibition was faster, inhibition was more intense, and duration of action was prolonged.
2 context sentences(design, population, supporting numbers)
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
Report a problemFND-1509359102
03AnimalAnimal study (in vivo)Efficacy outcome
In castrated male rats, increasing degarelix microparticle dose prolonged LH inhibition.
In plain wordsIn rats, increasing degarelix microparticle dose prolonged LH inhibition.
Peptide
Degarelix
Outcome
IncreaseDuration of LH inhibition with increasing dose
Study
ratn: not reported in source
castrated male rat
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
0.4, 1.0 and 1.5 mg/kgAs given in this study (rat).
Source sentences
Summary
When increasing the dose, onset of inhibition was faster, inhibition was more intense, and duration of action was prolonged.
2 context sentences(design, population, supporting numbers)
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
Report a problemFND-1509359103

Studies that did not test the peptide alone10

In this study, Degarelix 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 Degarelix.

04AnimalNot a test of Degarelix aloneAnimal study (in vivo)Efficacy outcome
In castrated male rats, spray-dried and microextrusion degarelix particles had comparable potencies.
In plain wordsIn rats, spray-dried and microextrusion degarelix particles had comparable potencies.
Peptide
Degarelix
Outcome
Direction not reportedPotency of spray-dried versus microextrusion particles
Study
ratn: not reported in source
castrated male rat
Comparator
microextrusion particles
Outcome group
Sex hormones and fertility · Endocrine and hormones
Source sentences
Summary
If spray-dried and microextrusion particles exhibited comparable potencies, double emulsion microspheres were significantly less potent, both for onset and duration of inhibition.
2 context sentences(design, population, supporting numbers)
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
In this study, Degarelix 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 Degarelix.
Report a problemFND-1509359104
05AnimalNot a test of Degarelix aloneAnimal study (in vivo)Efficacy outcome
In castrated male rats, double emulsion degarelix microspheres were significantly less potent for inhibition onset than spray-dried particles.
In plain wordsIn rats, double emulsion degarelix microspheres were less potent for inhibition onset than spray-dried particles.
Peptide
Degarelix
Outcome
DecreaseOnset potency of double emulsion microspheres versus spray-dried particles
Study
ratn: not reported in source
castrated male rat
Comparator
spray-dried particles
Outcome group
Sex hormones and fertility · Endocrine and hormones
Source sentences
Summary
If spray-dried and microextrusion particles exhibited comparable potencies, double emulsion microspheres were significantly less potent, both for onset and duration of inhibition.
2 context sentences(design, population, supporting numbers)
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
In this study, Degarelix 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 Degarelix.
Report a problemFND-1509359105
06AnimalNot a test of Degarelix aloneAnimal study (in vivo)Efficacy outcome
In castrated male rats, double emulsion degarelix microspheres were significantly less potent for inhibition onset than microextrusion particles.
In plain wordsIn rats, double emulsion degarelix microspheres were less potent for inhibition onset than microextrusion particles.
Peptide
Degarelix
Outcome
DecreaseOnset potency of double emulsion microspheres versus microextrusion particles
Study
ratn: not reported in source
castrated male rat
Comparator
microextrusion particles
Outcome group
Sex hormones and fertility · Endocrine and hormones
Source sentences
Summary
If spray-dried and microextrusion particles exhibited comparable potencies, double emulsion microspheres were significantly less potent, both for onset and duration of inhibition.
2 context sentences(design, population, supporting numbers)
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
In this study, Degarelix 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 Degarelix.
Report a problemFND-1509359106
07AnimalNot a test of Degarelix aloneAnimal study (in vivo)Efficacy outcome
In castrated male rats, double emulsion degarelix microspheres were significantly less potent for inhibition duration than spray-dried particles.
In plain wordsIn rats, double emulsion degarelix microspheres were less potent for inhibition duration than spray-dried particles.
Peptide
Degarelix
Outcome
DecreaseDuration potency of double emulsion microspheres versus spray-dried particles
Study
ratn: not reported in source
castrated male rat
Comparator
spray-dried particles
Outcome group
Sex hormones and fertility · Endocrine and hormones
Source sentences
Summary
If spray-dried and microextrusion particles exhibited comparable potencies, double emulsion microspheres were significantly less potent, both for onset and duration of inhibition.
2 context sentences(design, population, supporting numbers)
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
In this study, Degarelix 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 Degarelix.
Report a problemFND-1509359107
08AnimalNot a test of Degarelix aloneAnimal study (in vivo)Efficacy outcome
In castrated male rats, double emulsion degarelix microspheres were significantly less potent for inhibition duration than microextrusion particles.
In plain wordsIn rats, double emulsion degarelix microspheres were less potent for inhibition duration than microextrusion particles.
Peptide
Degarelix
Outcome
DecreaseDuration potency of double emulsion microspheres versus microextrusion particles
Study
ratn: not reported in source
castrated male rat
Comparator
microextrusion particles
Outcome group
Sex hormones and fertility · Endocrine and hormones
Source sentences
Summary
If spray-dried and microextrusion particles exhibited comparable potencies, double emulsion microspheres were significantly less potent, both for onset and duration of inhibition.
2 context sentences(design, population, supporting numbers)
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
In this study, Degarelix 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 Degarelix.
Report a problemFND-1509359108
09AnimalNot a test of Degarelix aloneAnimal study (in vivo)Efficacy outcome
In rats, increasing peptide content in degarelix microparticles shortened duration of action for all three particle types.
In plain wordsIn rats, increasing peptide content in degarelix microparticles shortened duration of action for all three particle types.
Peptide
Degarelix
Outcome
DecreaseDuration of action with increasing peptide content
Study
ratn: not reported in source
castrated male rat
Outcome group
Sex hormones and fertility · Endocrine and hormones
Source sentences
Summary
With the three types of particles, increasing peptide content was detrimental for duration of action, but only little difference was noticed between particles based on different polymers.
2 context sentences(design, population, supporting numbers)
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
In this study, Degarelix 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 Degarelix.
Report a problemFND-1509359111
10AnimalNot a test of Degarelix aloneAnimal study (in vivo)Efficacy outcome
In castrated male rats, degarelix particles based on different polymers showed little difference in duration of action.
In plain wordsIn rats, degarelix particles based on different polymers showed little difference in duration of action.
Peptide
Degarelix
Outcome
Direction not reportedEffect of polymer on duration of action
Study
ratn: not reported in source
castrated male rat
Comparator
particles based on different polymers
Outcome group
Sex hormones and fertility · Endocrine and hormones
Source sentences
Summary
With the three types of particles, increasing peptide content was detrimental for duration of action, but only little difference was noticed between particles based on different polymers.
2 context sentences(design, population, supporting numbers)
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
In this study, Degarelix 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 Degarelix.
Report a problemFND-1509359112
11AnimalNot a test of Degarelix aloneAnimal study (in vivo)Efficacy outcome
In castrated male rats, spray-dried degarelix microparticles inhibited LH for 36 days, exceeding unformulated degarelix by 1 week.
In plain wordsIn rats, spray-dried degarelix microparticles inhibited LH for 36 days, exceeding unformulated degarelix by 1 week.
Peptide
Degarelix
Outcome
IncreaseDuration of LH inhibition
Study
ratn: not reported in source
castrated male rat; spray-dried microparticles based on 75/25 lactate/glycolate copolymer
Comparator
unformulated degarelix at same dose
Outcome group
Sex hormones and fertility · Endocrine and hormones
Source sentences
Summary
At 1.5 mg/kg, LH inhibition was achieved over 36 days with spray-dried MP based on 75/25 lactate/glycolate copolymer.
3 context sentences(design, population, supporting numbers)
Summary · context
This was superior by 1 week to the performance of unformulated degarelix given at the same dose.
Summary · context
Poly (DL-lactide-co-glycolide) microparticles (MP) containing a highly potent peptidic gonadotropin releasing hormone antagonist (degarelix) of interest in the prostate cancer indication were screened for biological performance.
Summary · context
Efficacy was tested in a castrated male rat model at 3 doses (0.4, 1.0 and 1.5 mg/kg) and assessed as inhibition of luteinizing hormone (LH) secretion.
In this study, Degarelix 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 Degarelix.
Report a problemFND-1509359113
12LabNot a test of Degarelix aloneIn vitro (cell-free)Other
In formulation tests, double emulsion microspheres released significantly less degarelix upon reconstitution, maximum 0.3%, versus maximum 2% for spray-dried microparticles.
In plain wordsIn lab tests, double emulsion microspheres released less degarelix upon reconstitution than spray-dried microparticles.
Peptide
Degarelix
Outcome
DecreaseReleased fraction versus spray-dried microparticles
Study
n: not reported in source
microparticle reconstitution
Comparator
spray-dried microparticles
Outcome group
Pharmacokinetics · Pharmacology
Source sentences
Summary
Interestingly, for the latter type it was found that the degarelix fraction released upon reconstitution in the solution for injection was significantly lower (max 0.3%), in comparison to spray-dried MP (max 2%) or microextrusion (max 4%).
In this study, Degarelix 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 Degarelix.
Report a problemFND-1509359109
13LabNot a test of Degarelix aloneIn vitro (cell-free)Other
In formulation tests, double emulsion microspheres released significantly less degarelix upon reconstitution, maximum 0.3%, versus maximum 4% for microextrusion microparticles.
In plain wordsIn lab tests, double emulsion microspheres released less degarelix upon reconstitution than microextrusion microparticles.
Peptide
Degarelix
Outcome
DecreaseReleased fraction versus microextrusion microparticles
Study
n: not reported in source
microparticle reconstitution
Comparator
microextrusion microparticles
Outcome group
Pharmacokinetics · Pharmacology
Source sentences
Summary
Interestingly, for the latter type it was found that the degarelix fraction released upon reconstitution in the solution for injection was significantly lower (max 0.3%), in comparison to spray-dried MP (max 2%) or microextrusion (max 4%).
In this study, Degarelix 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 Degarelix.
Report a problemFND-1509359110

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, 16:34 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

Publication types

Journal Article

MeSH terms

PepBank is a research reference. Talk to a doctor before you use any peptide.