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Preparation of Cross-Linked Sodium Alginate Microspheres with Different Metal Ions Using the Microfluidic Electrospray Technology

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A new method of preparing TRH derivative-loaded poly(dl-lactide-coglycolide) microspheres based on a solid solution

A Matsumoto¹, Y Matsukawa, Y Nishioka

¹Tanabe Seiyaku Co., Ltd., Osaka, Japan.

Drug Discoveries & Therapeutics

|April 17, 2012

Summary

This study introduces a novel solid solution method for creating peptide-loaded poly(dl-lactide-co-glycolide) microspheres. This technique achieves high encapsulation efficiency and sustained peptide release over 21 days with minimal initial burst.

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Last Updated: May 23, 2026

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Area of Science:

Biomaterials Science
Drug Delivery Systems
Polymer Chemistry

Background:

Poly(dl-lactide-co-glycolide) (PLGA) microspheres are widely used for sustained drug delivery.
Achieving high encapsulation efficiency and controlled release profiles remains a challenge.
Novel preparation methods are needed to improve peptide loading and release characteristics.

Purpose of the Study:

To develop and evaluate a new method for preparing peptide-loaded PLGA microspheres.
To achieve high encapsulation efficiency, low initial burst, and long-term sustained release of peptides.
To investigate the effect of a solid solution system on peptide dispersion and release.

Main Methods:

Preparation of solid solutions by dissolving PLGA and a TRH derivative peptide in mixed solvents.
Fabrication of microspheres using an oil-in-water (O/W) emulsion solvent evaporation method with the solid solution in dichloromethane as the oil phase.
Characterization of peptide state using X-ray diffraction (XRD) and Differential Scanning Calorimetry (DSC) analysis.
Evaluation of in vitro peptide release profiles.

Main Results:

Peptides were found to be molecularly dispersed in the solid solution and PLGA microspheres up to 15% peptide loading.
Encapsulation efficiency exceeded 90% for microspheres with peptide loading up to 15%.
In vitro release studies demonstrated sustained peptide release over 21 days with a significantly reduced initial burst.

Conclusions:

The solid solution system is effective for preparing peptide-loaded PLGA microspheres.
This method successfully enhances encapsulation efficiency and achieves long-term sustained peptide release.
The developed microspheres show potential for advanced therapeutic applications requiring controlled peptide delivery.