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<p>The Food and Drug Administration of the United States (USFDA) and the European Medicines Agency (EMA) have approved peptide-based long-acting formulations to manage chronic diseases. However, the formulation of long-acting injectables for hydrophilic drug molecules and peptides remains a persistent challenge due to poor encapsulation and high initial burst release, which increases the complexity of the formulation. In the present research, we formulated long-acting injectable microspheres for liraglutide, a peptide used for managing type 2 DM (Diabetes Mellitus), utilizing a modified solid-oil–water (S/O/W) method. The method includes a hydrophobic ion pairing (HIP) strategy to improve the hydrophobicity of native molecules using various hydrophobic ion-pairing agents. Further, the PLGA microspheres prepared by the modified S/O/W method were compared with the traditional water–oil-water (W/O/W) double emulsion method. The modified S/O/W method (batch F2) demonstrated a significant improvement in encapsulation efficiency, increasing from 56.15% to 85.45%, and a minimal burst release of 3.58%. A comprehensive characterization of microspheres was performed using modern analytical techniques. The developed microspheres were spherical with a mean particle size of 43.97&#xa0;µm and exhibited sustained drug release over 55&#xa0;days. The S/O/W method demonstrated a promising approach for the encapsulation of hydrophilic peptide molecules.</p> Graphical Abstract <p></p>

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Influence of Hydrophobic Ion Pairing on Formulation Performance of Liraglutide in PLGA Microspheres

  • 期刊论文

  • 发表日期：

    2025年7月29日

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  • Jyotsna G. Vitore,
  • Varla Yalamanda,
  • Devendra Singh Tomar,
  • Satish Rojekar,
  • Dhwani Rana,
  • Derajram Benival

摘要

The Food and Drug Administration of the United States (USFDA) and the European Medicines Agency (EMA) have approved peptide-based long-acting formulations to manage chronic diseases. However, the formulation of long-acting injectables for hydrophilic drug molecules and peptides remains a persistent challenge due to poor encapsulation and high initial burst release, which increases the complexity of the formulation. In the present research, we formulated long-acting injectable microspheres for liraglutide, a peptide used for managing type 2 DM (Diabetes Mellitus), utilizing a modified solid-oil–water (S/O/W) method. The method includes a hydrophobic ion pairing (HIP) strategy to improve the hydrophobicity of native molecules using various hydrophobic ion-pairing agents. Further, the PLGA microspheres prepared by the modified S/O/W method were compared with the traditional water–oil-water (W/O/W) double emulsion method. The modified S/O/W method (batch F2) demonstrated a significant improvement in encapsulation efficiency, increasing from 56.15% to 85.45%, and a minimal burst release of 3.58%. A comprehensive characterization of microspheres was performed using modern analytical techniques. The developed microspheres were spherical with a mean particle size of 43.97 µm and exhibited sustained drug release over 55 days. The S/O/W method demonstrated a promising approach for the encapsulation of hydrophilic peptide molecules.

Graphical Abstract