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<p>The emergence and widespread distribution of multidrug-resistant bacteria have raised serious public health concerns and led to significant negative impacts on clinical outcomes, healthcare costs, and public health strategies worldwide. The development of pharmaceuticals capable of effectively combating bacterial infections represents a significant challenge for contemporary medical science. In this article, delivery systems in the form of micro- and nanoparticles based on biodegradable poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) containing novel 1-antipyryl-1<i>H</i>-pyrrol-2-one (NAP) were prepared and characterized in terms of their hydrodynamic size, zeta potential, surface morphology, encapsulation efficiency, drug loading, and structural characteristics. For particles possessing the best characteristics, in vitro drug release pattern, thermal properties, cytocompatibility with C2C12 myoblasts and hemolytic activity were determined. The obtained micro- and nanoparticles had regular spherical shape, average diameter of 1350–5763&#xa0;nm (for microparticles) and 553–745&#xa0;nm (for nanoparticles), and zeta potential ranging from  −&#xa0;43.9 mV to −&#xa0;25.5 mV. The encapsulation of NAP into the PHBV matrix led to a decrease in degradation temperature and an increase in particle size, cold crystallization and glass transition temperatures in comparison with empty particles. The in vitro release study revealed that the release of NAP from PHBV particles followed the Fickian diffusion-controlled mechanism; the maximum cumulative amount of NAP (66.8%) in the studied medium was achieved in 120&#xa0;h. Neither pristine NAP nor NAP-loaded PHBV microparticles influenced the metabolic activity and membrane integrity of C2C12 cells and caused haemoglobin leakage from human red blood cells (RBCs). Therefore, the obtained NAP-loaded PHBV microparticles may be suitable for sustained intramuscular delivery of NAP.</p>

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Delivery Systems of Novel 1-Antipyryl-1H-Pyrrol-2-One Based on Polyhydroxyalkanoate Micro- and Nanoparticles: Preparation, Characterization and in Vitro Cytocompatibility Assay

  • 期刊论文

  • 发表日期：

    2026年3月24日

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  • Sergei Y. Lipaikin,
  • Aleksei S. Dorokhin,
  • Galina A. Ryltseva,
  • Andrey V. Oberenko,
  • Evgeniy G. Kiselev,
  • Alexander V. Shabanov,
  • Vadim A. Lyadov,
  • Nika V. Shavrina,
  • Alexander O. Terent’ev,
  • Sabu Thomas,
  • Tatiana G. Volova,
  • Cathrine Kessler

摘要

The emergence and widespread distribution of multidrug-resistant bacteria have raised serious public health concerns and led to significant negative impacts on clinical outcomes, healthcare costs, and public health strategies worldwide. The development of pharmaceuticals capable of effectively combating bacterial infections represents a significant challenge for contemporary medical science. In this article, delivery systems in the form of micro- and nanoparticles based on biodegradable poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) containing novel 1-antipyryl-1H-pyrrol-2-one (NAP) were prepared and characterized in terms of their hydrodynamic size, zeta potential, surface morphology, encapsulation efficiency, drug loading, and structural characteristics. For particles possessing the best characteristics, in vitro drug release pattern, thermal properties, cytocompatibility with C2C12 myoblasts and hemolytic activity were determined. The obtained micro- and nanoparticles had regular spherical shape, average diameter of 1350–5763 nm (for microparticles) and 553–745 nm (for nanoparticles), and zeta potential ranging from  − 43.9 mV to − 25.5 mV. The encapsulation of NAP into the PHBV matrix led to a decrease in degradation temperature and an increase in particle size, cold crystallization and glass transition temperatures in comparison with empty particles. The in vitro release study revealed that the release of NAP from PHBV particles followed the Fickian diffusion-controlled mechanism; the maximum cumulative amount of NAP (66.8%) in the studied medium was achieved in 120 h. Neither pristine NAP nor NAP-loaded PHBV microparticles influenced the metabolic activity and membrane integrity of C2C12 cells and caused haemoglobin leakage from human red blood cells (RBCs). Therefore, the obtained NAP-loaded PHBV microparticles may be suitable for sustained intramuscular delivery of NAP.