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Pharmaceutical Research

, 35:62 | Cite as

Progesterone PLGA/mPEG-PLGA Hybrid Nanoparticle Sustained-Release System by Intramuscular Injection

  • Bin Xie
  • Yang Liu
  • Yuting Guo
  • Enbo Zhang
  • Chenguang Pu
  • Haibing He
  • Tian Yin
  • Xing Tang
Research Paper

Abstract

Purpose

To prepare sustained-release PLGA/mPEG-PLGA hybrid nanoparticles of progesterone (PRG), and evaluate the descending required administration dosage in vivo.

Methods

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.

Results

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.

Conclusions

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 Words

in vivo PEGylated PLGA/mPEG-PLGA progesterone sustained release 

Abbreviations

AUC0-t

Area under the curve from time 0 to the last observed concentration time

BP

Phenylcarbinol

Cmax

Maximum serum concentration

DDS

Drug delivery systems

DL

Drug loading

DLS

Dynamic light scattering

DSC

Differential scanning calorimetry

EA

Ethyl acetate

F68

Pluronic F68

i.m.

Intramuscular

LC–MS/MS

Liquid chromatography–mass spectrometry/mass spectrometry

mPEG-PLGA

Methoxy poly (ethylene glycol)-poly(ε-caprolactone)

MRT

Mean retention time

MS

Microspheres

Mw

Molecular weight

NPs

Nanoparticles

PBS

Phosphate buffered saline

PLGA

Poly D, L-lactic-co-glycolic acid

PRG

Progesterone

SD

Sprague-dawley

t1/2

Half-life

TEM

Transmission electron microscopy

Notes

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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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  • Bin Xie
    • 1
  • Yang Liu
    • 1
  • Yuting Guo
    • 1
  • Enbo Zhang
    • 1
  • Chenguang Pu
    • 1
  • Haibing He
    • 1
  • Tian Yin
    • 1
  • Xing Tang
    • 1
  1. 1.School of PharmacyShenyang Pharmaceutical UniversityShenyangChina

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