KIT-6介孔材料修饰的不对称聚醚砜膜增强阿奇霉素的传递:优化及机理研究

IF 4.7 3区 医学 Q1 PHARMACOLOGY & PHARMACY European Journal of Pharmaceutical Sciences Pub Date : 2025-04-01 Epub Date: 2025-02-09 DOI:10.1016/j.ejps.2025.107038
Mahya Samari , Soheila Kashanian , Sirus Zinadini , Hossein Derakhshankhah
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引用次数: 0

摘要

本研究提出了一种新型药物递送系统的开发,旨在改善阿奇霉素(AZI)的释放特征和持续递送,特别是针对需要局部感染控制和改善组织相容性的应用。该系统采用KIT-6介孔材料修饰的不对称聚醚砜(PES)膜,与传统的给药平台相比,具有更好的药物释放性能和生物相容性。通过系统地改变膜厚度(150 ~ 600µm)、药物浓度(500 ~ 1500 mg/L)、聚合物含量(13 ~ 21% PES)、造孔剂百分比(0 ~ 4%聚乙烯吡罗烷酮)和KIT-6改性剂百分比(0.5 ~ 2%)等参数,对膜进行优化。表征包括扫描电子显微镜、水接触角测量、孔隙度、拉伸强度评估和综合生物活性测试(细胞毒性、抗菌功效、血液相容性和一种新的组织完整性检测)。与未修饰膜(252 mg/L)相比,优化后的配方(17% PES, 2% PVP, 1% KIT-6)具有更好的药物利用度(464 mg/L),缓释谱符合Higuchi模型。此外,体外和离体研究证明,该膜具有优越的生物相容性(约90%的细胞活力,1.2%的低溶血率),并且比未修饰的膜更好地保存了组织完整性。值得注意的是,该系统在长期使用中显示出强大的可重复使用性,这表明它有潜力成为一种有效、可持续和生物相容性的局部AZI递送解决方案。这些优点使该系统成为需要精确药物释放和最小组织破坏的医疗应用的有希望的替代方案。
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Enhanced delivery of azithromycin using asymmetric polyethersulfone membrane modified with KIT-6 mesoporous material: Optimization and mechanistic studies
This study presents the development of a novel drug delivery system designed for improving the release profile and sustained delivery of azithromycin (AZI), particularly aimed at applications requiring localized infection control and improved tissue compatibility. The system employs an asymmetric polyethersulfone (PES) membrane modified with KIT-6 mesoporous material, offering improved drug release performance and biocompatibility over conventional delivery platforms. Membrane optimization was achieved by systematically varying parameters such as thickness (150–600 µm), drug concentration (500–1500 mg/L), polymer content (13–21 % PES), pore maker percentage (0–4 % polyvinylpyrrolidone), and KIT-6 modifier percentage (0.5–2 %). Characterization included scanning electron microscopy, water contact angle measurements, porosity, tensile strength evaluation, and comprehensive bioactivity testing (cytotoxicity, antimicrobial efficacy, blood compatibility, and a novel tissue integrity assay).
The optimized formulation (17 % PES, 2 % PVP, 1 % KIT-6) achieved a controlled and sustained release profile with improved drug availability (464 mg/L) compared to unmodified membranes (252 mg/L), with a sustained release profile governed by the Higuchi model. Additionally, the membrane demonstrated superior biocompatibility (–90 % cell viability, low hemolysis at 1.2 %) and preserved tissue integrity better than unmodified counterparts, as evidenced by in vitro and ex vivo studies. Notably, the system showed robust reusability over prolonged use, indicating its potential as an effective, sustainable, and biocompatible solution for localized AZI delivery. These advantages position this system as a promising alternative for medical applications requiring precise drug release and minimal tissue disruption.
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CiteScore
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期刊介绍: The journal publishes research articles, review articles and scientific commentaries on all aspects of the pharmaceutical sciences with emphasis on conceptual novelty and scientific quality. The Editors welcome articles in this multidisciplinary field, with a focus on topics relevant for drug discovery and development. More specifically, the Journal publishes reports on medicinal chemistry, pharmacology, drug absorption and metabolism, pharmacokinetics and pharmacodynamics, pharmaceutical and biomedical analysis, drug delivery (including gene delivery), drug targeting, pharmaceutical technology, pharmaceutical biotechnology and clinical drug evaluation. The journal will typically not give priority to manuscripts focusing primarily on organic synthesis, natural products, adaptation of analytical approaches, or discussions pertaining to drug policy making. Scientific commentaries and review articles are generally by invitation only or by consent of the Editors. Proceedings of scientific meetings may be published as special issues or supplements to the Journal.
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