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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 Full article

Journal Journal of Polymers and the Environment
ISSN: 1572-8919
Output data Year: 2026, Volume: 34, Number: 4, Article number : 79, Pages count : DOI: 10.1007/s10924-026-03769-8
Authors Lipaikin Sergei Y. 1 , Dorokhin Aleksei S. 2,1 , Ryltseva Galina A. 2,1 , Oberenko Andrey V. 1 , Kiselev Evgeniy G. 2,1 , Shabanov Alexander V. 3 , Lyadov Vadim A. 4 , Shavrina Nika V. 4 , Terent’ev Alexander O. 5 , Thomas Sabu 6,7 , Volova Tatiana G. 2,1 , Kessler Cathrine 2,1
Affiliations
1 Siberian Federal University, 79 Svobodny pr., Krasnoyarsk, 660041, Russia
2 Institute of Biophysics SB RAS, Federal Research Center “Krasnoyarsk Science Center SB RAS”, 50/50 Akademgorodok, Krasnoyarsk, 660036, Russia
3 L.V. Kirensky Institute of Physics, Siberian Branch of the Russian Academy of Sciences, 50/12 Akademgorodok, Krasnoyarsk, 660036, Russia
4 Perm National Research Polytechnic University, 29 Komsomolsky ave., Perm, 614990, Russia
5 N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 47 Leninsky prosp., Moscow, 119991, Russia
6 Department of Chemical Sciences, University of Johannesburg, Doornfontein, P.O. Box 17011, Johannesburg, 2028, South Africa
7 International and Inter University Centre for Nanoscience and Nanotechnology, School of Energy Materials, and School of Nanoscience and Nanotechnology, Mahatma Gandhi University, Kottayam, 686 560, Kerala, India

Abstract: 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.
Cite: Lipaikin S.Y. , Dorokhin A.S. , Ryltseva G.A. , Oberenko A.V. , Kiselev E.G. , Shabanov A.V. , Lyadov V.A. , Shavrina N.V. , Terent’ev A.O. , Thomas S. , Volova T.G. , Kessler C.
Delivery Systems of Novel 1-Antipyryl-1H-Pyrrol-2-One Based on Polyhydroxyalkanoate Micro- and Nanoparticles: Preparation, Characterization and in Vitro Cytocompatibility Assay
Journal of Polymers and the Environment. 2026. V.34. N4. 79 . DOI: 10.1007/s10924-026-03769-8 WOS Scopus OpenAlex
Dates:
Submitted: Sep 16, 2025
Published online: Mar 24, 2026
Identifiers:
≡ Web of science: WOS:001722932600005
≡ Scopus: 2-s2.0-105034943276
≡ OpenAlex: W7140160355
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