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首页> 外文期刊>International immunopharmacology >In vivo anti-apoptosis activity of novel berberine-loaded chitosan nanoparticles effectively ameliorates osteoarthritis
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In vivo anti-apoptosis activity of novel berberine-loaded chitosan nanoparticles effectively ameliorates osteoarthritis

机译：新型黄连素负载壳聚糖纳米粒的体内抗凋亡活性可有效改善骨关节炎

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摘要

Berberine chloride (BBR) is an isoquinoline alkaloid that possesses promising protective efficacies against osteoarthritis (OA). Nevertheless, the therapeutic agent of this substance in OA is limited by its poor aqueous solubility, low bioavailability and short biological half-life. In this study, chitosan (CS)-based nanoparticles were prepared for the sustained release of BBR. Novel BBR-loaded chitosan nanoparticles (CNs) were successfully synthesized by the ionic cross-linking method. BBR-loaded CNs were spherical and homogeneous in shape. Moreover, they exhibited good stability and had ideal releasing profile in vitro. After intra-articular injection of BBR-loaded CNs, the level of BBR in rat plasma decreased and the retention time in synovial fluid increased compared with free BBR solution. In vivo evaluation of BBR-loaded CNs further showed higher anti-apoptosis activity in the treatment of OA compared with BBR solution at equivalent concentration. This result was evidenced by the changes of gross morphology and histological analyses in rat articular cartilage, TUNEL assay, quantitative real-time polymerase chain reaction, Western blot, and immunohistochemical analyses of caspase-3, Bcl-2 and Bax expressions. Given these results, BBR-loaded CNs are potential therapeutic agents for OA (C) 2015 Elsevier B.V. All rights reserved.
机译：氯化小ber碱（BBR）是一种异喹啉生物碱，具有抗骨关节炎（OA）的有前途的保护作用。然而，该物质在OA中的治疗剂由于其水溶性差，生物利用度低和生物半衰期短而受到限制。在这项研究中，制备基于壳聚糖（CS）的纳米颗粒以持续释放BBR。通过离子交联方法成功合成了新型负载BBR的壳聚糖纳米粒子（CN）。负载BBR的CN为球形，形状均匀。此外，它们表现出良好的稳定性并且在体外具有理想的释放特性。关节内注射负载BBR的CNs后，与游离BBR溶液相比，大鼠血浆中BBR的水平降低，滑液中的保留时间增加。与同等浓度的BBR溶液相比，BBR负载的CNs的体内评估进一步显示了在OA治疗中具有更高的抗凋亡活性。大鼠关节软骨的总体形态学和组织学分析的变化，TUNEL测定法，定量实时聚合酶链反应，蛋白质印迹以及caspase-3，Bcl-2和Bax表达的免疫组织化学分析证明了这一结果。鉴于这些结果，负载BBR的CN是OA（C）2015 Elsevier B.V.的潜在治疗剂。保留所有权利。

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