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用于厚朴酚与和厚朴酚药物制剂的β-环糊精-低聚丙交酯无聚合物静电纺丝法

Polymer-Free Electrospinning of β-Cyclodextrin-Oligolactide for Magnolol and Honokiol Pharmaceutical Formulations.

作者信息

Blaj Diana-Andreea, Peptu Catalina A, Balan-Porcarasu Mihaela, Peptu Cristian, Tuchilus Cristina Gabriela, Ochiuz Lacramioara

机构信息

"Petru Poni" Institute of Macromolecular Chemistry, 700487 Iasi, Romania.

Faculty of Chemical Engineering and Protection of the Environment, "Gheorghe Asachi" Technical University of Iasi, 700050 Iasi, Romania.

出版信息

Pharmaceutics. 2025 Jan 17;17(1):130. doi: 10.3390/pharmaceutics17010130.

DOI:10.3390/pharmaceutics17010130
PMID:39861776
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11768894/
Abstract

Magnolol (MG) and honokiol (HK) are bioactive compounds extracted from and trees with significant pharmacological properties, including antioxidant and antibacterial activity. However, their poor water solubility and low bioavailability limit the therapeutic potential. To address these limitations, this study aims to develop MG and HK formulations by co-electrospinning using custom-synthesized β-cyclodextrin-oligolactide (β-CDLA) derivatives. MALDI MS and NMR were employed for the structural assessment of the β-CDLA derivatives. This polymer-free electrospinning technique utilizes the high solubility of β-CDLA to incorporate MG and HK into fibrous webs. The morphology of the resulting fibers is established by SEM and further characterized using FTIR and NMR spectroscopy to confirm the successful incorporation of MG and HK. The antioxidant activity was determined using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay, while the antimicrobial activity was evaluated against several standard microorganisms (, , , and ). The MG and HK electrospun formulations were prepared using highly concentrated feed solutions in dimethylformamide (180% w/v). The resulting β-CDLA fibers, with diameters above 400 nm and an active compound content of 7% wt., exhibited enhanced long-term antioxidant activity and improved antimicrobial efficacy, including notable activity against . This study demonstrates the potential of MG and HK-loaded β-CDLA fibrous formulations as delivery systems with prolonged antioxidant activity and notable antibacterial efficacy, providing a promising platform for biomedical applications.

摘要

厚朴酚(MG)和和厚朴酚(HK)是从厚朴树和凹叶厚朴树中提取的生物活性化合物,具有显著的药理特性,包括抗氧化和抗菌活性。然而,它们较差的水溶性和低生物利用度限制了其治疗潜力。为了解决这些限制,本研究旨在通过使用定制合成的β-环糊精-低聚丙交酯(β-CDLA)衍生物进行共电纺丝来开发MG和HK制剂。采用基质辅助激光解吸电离质谱(MALDI MS)和核磁共振(NMR)对β-CDLA衍生物进行结构评估。这种无聚合物的电纺丝技术利用β-CDLA的高溶解性将MG和HK纳入纤维网中。通过扫描电子显微镜(SEM)确定所得纤维的形态,并进一步使用傅里叶变换红外光谱(FTIR)和核磁共振光谱进行表征,以确认MG和HK的成功掺入。使用2,2-二苯基-1-苦基肼基(DPPH)自由基清除试验测定抗氧化活性,同时针对几种标准微生物(金黄色葡萄球菌、大肠杆菌、白色念珠菌和黑曲霉)评估抗菌活性。MG和HK电纺制剂使用二甲基甲酰胺中的高浓度进料溶液(180% w/v)制备。所得的β-CDLA纤维直径超过400 nm,活性化合物含量为7% wt.,表现出增强的长期抗氧化活性和改善的抗菌功效,包括对金黄色葡萄球菌的显著活性。本研究证明了负载MG和HK的β-CDLA纤维制剂作为具有延长抗氧化活性和显著抗菌功效的递送系统的潜力,为生物医学应用提供了一个有前景的平台。

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本文引用的文献

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Enrofloxacin Pharmaceutical Formulations through the Polymer-Free Electrospinning of β-Cyclodextrin-oligolactide Derivatives.通过β-环糊精-低聚丙交酯衍生物的无聚合物静电纺丝制备恩诺沙星药物制剂。
Pharmaceutics. 2024 Jul 5;16(7):903. doi: 10.3390/pharmaceutics16070903.
2
Synthesis of β-cyclodextrin derivatives substituted at larger or smaller rims via amine-catalyzed ring-opening oligomerization of ε-caprolactone.通过ε-己内酯的胺催化开环低聚反应合成在较大或较小边缘被取代的β-环糊精衍生物。
Carbohydr Polym. 2024 Jun 15;334:122032. doi: 10.1016/j.carbpol.2024.122032. Epub 2024 Mar 7.
3
Magnolol Loaded on Carboxymethyl Chitosan Particles Improved the Antimicrobial Resistance and Storability of Kiwifruits.
负载于羧甲基壳聚糖颗粒上的厚朴酚提高了猕猴桃的抗菌性和耐贮性。
Foods. 2023 Mar 8;12(6):1149. doi: 10.3390/foods12061149.
4
Electrospinning of Cyclodextrin-Oligolactide Derivatives.环糊精低聚物衍生物的静电纺丝。
Biomolecules. 2023 Jan 19;13(2):203. doi: 10.3390/biom13020203.
5
pH-responsive magnolol nanocapsule-embedded magnolol-grafted-chitosan hydrochloride hydrogels for promoting wound healing.pH 响应性厚朴酚纳米胶囊嵌入的厚朴酚接枝壳聚糖盐酸盐水凝胶促进伤口愈合。
Carbohydr Polym. 2022 Sep 15;292:119643. doi: 10.1016/j.carbpol.2022.119643. Epub 2022 May 20.
6
Magnolol Hybrid Nanofibrous Mat with Antibacterial, Anti-Inflammatory, and Microvascularized Properties for Wound Treatment.具有抗菌、抗炎和微血管化特性的厚朴酚混合纳米纤维垫用于伤口治疗。
Biomacromolecules. 2022 Mar 14;23(3):1124-1137. doi: 10.1021/acs.biomac.1c01430. Epub 2022 Jan 23.
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Development of Membrane-Active Honokiol/Magnolol Amphiphiles as Potent Antibacterial Agents against Methicillin-Resistant (MRSA).膜活性和厚朴酚/厚朴酚两亲体的开发作为对抗耐甲氧西林金黄色葡萄球菌(MRSA)的有效抗菌剂。
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