使用新型生物相容性依托妥昔布壳聚糖-透明质酸混合微粒在关节内治疗骨关节炎。

IF 3 4区医学 Q2 CHEMISTRY, APPLIED

Journal of microencapsulation Pub Date : 2025-06-01 Epub Date: 2025-04-17 DOI:10.1080/02652048.2025.2490033

Khaled E Abuelella, Hend Abd-Allah, Sara M Soliman, Mona M A Abdel-Mottaleb

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引用次数: 0

摘要

目的：目前的研究旨在开发和评估依托妥昔布（ETX）负载的多电解质微颗粒（PEMPs）在骨关节炎治疗中的关节内给药。方法：利用透明质酸（HA）与壳聚糖（CS）之间的静电相互作用制备质子交换膜。通过包封率、粒径（PS）、ζ电位（ZP）、药物释放度、稳定性、透射电镜（TEM）、红外光谱（FTIR）、DSC和体内抗炎活性等指标对其进行表征。结果：最佳配方（ME4/TPP0.25）为球形颗粒，PS为1.56±0.04µm， PDI为0.29±0.05，ZP为+35.26±0.9 mV， EE%为94.7±0.24%，载药量为11.7±0.16% （w/w）。体内研究表明，与单独用药相比，ME4/TPP0.25可显著抑制膝关节肿胀，并显著降低分解代谢和炎症介质（ALP和IL-6）的水平。结论：这些结果表明，最佳的etx负载PEMPs可能是治疗膝关节骨关节炎的有希望的配方。

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Intra-articular treatment of osteoarthritis using novel biocompatible etoricoxib chitosan-hyaluronate hybrid microparticles.

Aim: The current study aimed to develop and evaluate Etoricoxib (ETX) loaded polyelectrolyte microparticles (PEMPs) for intra-articular delivery in osteoarthritis management.

Methods: PEMPs were prepared by the electrostatic interactions between hyaluronic acid (HA) and chitosan (CS). The optimum formulation was characterized for encapsulation efficiency, particle size (PS), zeta potential (ZP), drug release, stability, TEM, FTIR, DSC and in vivo anti-inflammatory activity.

Results: The optimum formulation (ME4/TPP0.25) demonstrated spherical particles with a PS of 1.56 ± 0.04 µm, a PDI value of 0.29 ± 0.05, ZP of +35.26 ± 0.9 mV, and EE% of 94.7 ± 0.24% and loading capacity of 11.7 ± 0.16% (w/w). In vivo studies demonstrated that ME4/TPP0.25 significantly suppressed knee joint swelling, and significantly reduced the levels of catabolic and inflammatory mediators (ALP and IL-6) compared to drug alone.

Conclusion: These results suggest that the optimum ETX-loaded PEMPs could be a promising formulation for knee osteoarthritis management.

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来源期刊

Journal of microencapsulation 工程技术-工程：化工

CiteScore

6.30

自引率

2.60%

发文量

审稿时长

3 months

期刊介绍： The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.