Progesterone PLGA/mPEG-PLGA Hybrid Nanoparticle Sustained-Release System by Intramuscular Injection
To prepare sustained-release PLGA/mPEG-PLGA hybrid nanoparticles of progesterone (PRG), and evaluate the descending required administration dosage in vivo.
PRG hybrid nanoparticles (PRG H-NPs) based on PLGA/mPEG-PLGA were compared with PRG nanoparticles (PRG-NPs) of pure PLGA as the matrix and PRG-oil solutions. Nanoparticles (NPs) were formed by the method of nanoemulsion, and the pharmacokinetics of the sustained-release PRG H-NPs in male Sprague dawley (SD) rats were investigated. The rats were randomly divided into four groups, each group received: single dose of PRG H-NPs (14.58 mg/kg, i.m.) and PRG-NPs (14.58 mg/kg, i.m.), repeated dosing for 7 days of PRG-oil (2.08 mg/kg, i.m.) solution (Oil-L) and a higher dosage of PRG-oil (6.24 mg/kg, i.m.) solution (Oil-H), respectively.
In the pharmacokinetic test, the PRG H-NPs exhibited a comparatively good sustained-release effect against the PRG-NPs without mPEG-PLGA and PRG-oil solution. The pharmacokinetic parameters of the PRG H-NPs, PRG-NPs, Oil-L and Oil-H were AUC0–t(ng·h·mL−1) 8762.1, 1546.1, 1914.5, and 12,138.9, t1/2 (h)52.7, 44.1, 8.4 and 44.6 respectively.
Owing to the modification of PEG, PRG H-NPs can act as safe delivery platforms for sustained-release of drugs with a lower dosage required.
Key Wordsin vivo PEGylated PLGA/mPEG-PLGA progesterone sustained release
Area under the curve from time 0 to the last observed concentration time
Maximum serum concentration
Drug delivery systems
Dynamic light scattering
Differential scanning calorimetry
Liquid chromatography–mass spectrometry/mass spectrometry
Methoxy poly (ethylene glycol)-poly(ε-caprolactone)
Mean retention time
Phosphate buffered saline
Poly D, L-lactic-co-glycolic acid
Transmission electron microscopy
Acknowledgments and Disclosures
This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors. The authors have declared no conflicts of interest. All the experiments reported comply with European Federation of Pharmaceutical Industries Associations.
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