Șerban Alexandru-Mihail, Nacu Isabella, Rosca Irina, Ghilan Alina, Rusu Alina Gabriela, Niță Loredana Elena, Darie-Niță Raluca Nicoleta, Chiriac Aurica P
Department of Natural Polymers, Bioactive and Biocompatible Materials, "Petru Poni" Institute of Macromolecular Chemistry, 41-A Grigore Ghica Voda Alley, 700487 Iasi, Romania.
Biomedical Sciences Department, Faculty of Medical Bioengineering, Grigore T. Popa University of Medicine and Pharmacy of Iasi, 9-13 Kogalniceanu Street, 700454 Iasi, Romania.
Pharmaceutics. 2024 Apr 17;16(4):550. doi: 10.3390/pharmaceutics16040550.
In recent years, increasing interest has been accorded to polyester-based polymer microstructures, driven by their promising potential as advanced drug delivery systems. This study presents the preparation and characterization of new polymeric microparticles based on poly(ethylene brassylate-co-squaric acid) loaded with norfloxacin, a broad-spectrum antibiotic. Polymacrolactone was synthesised in mild conditions through the emulsion polymerization of bio-based and renewable monomers, ethylene brassylate, and squaric acid. The microparticles were obtained using the precipitation technique and subsequently subjected to comprehensive characterization. The impact of the copolymer/drug ratio on various properties of the new system was systematically evaluated, confirming the structure of the copolymer and the encapsulation of norfloxacin. The microspheres are approximately spherical and predominantly homogeneously distributed. The average hydrodynamic diameter of the microparticles falls between 400 and 2000 nm, a decrease that is observed with the increase in norfloxacin content. All samples showed good encapsulation efficiency and drug loading capacity, with the highest values obtained for microparticles synthesised using an equal ratio of copolymer and drug. In vitro drug release results disclose that norfloxacin molecules are released in a sustained biphasic manner for up to 24 h. Antimicrobial activity was also studied, with samples showing very good activity against and moderate activity against and . In addition, HDFA human fibroblast cell cultures demonstrated the cytocompatibility of the microparticles.
近年来，聚酯基聚合物微结构因其作为先进药物递送系统的潜在前景而受到越来越多的关注。本研究介绍了负载广谱抗生素诺氟沙星的聚（乙二酸癸二醇酯 - 共 - 方酸）新型聚合物微粒的制备与表征。聚（乙二酸癸二醇酯 - 共 - 方酸）是通过生物基可再生单体乙二酸癸二醇酯和方酸的乳液聚合在温和条件下合成的。使用沉淀技术获得微粒，随后对其进行全面表征。系统评估了共聚物/药物比例对新系统各种性能的影响，证实了共聚物的结构以及诺氟沙星的包封情况。微球近似球形，且主要均匀分布。微粒的平均流体动力学直径在400至2000纳米之间，随着诺氟沙星含量的增加，该直径会减小。所有样品均显示出良好的包封效率和载药能力，使用共聚物与药物等比例合成的微粒获得了最高值。体外药物释放结果表明，诺氟沙星分子以持续双相方式释放长达24小时。还研究了抗菌活性，样品对[具体菌种1]显示出非常好的活性，对[具体菌种2]和[具体菌种3]显示出中等活性。此外，人成纤维细胞HDFA培养物证明了微粒的细胞相容性。
