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首页> 外文期刊>Journal of Controlled Release: Official Journal of the Controlled Release Society >Prolonged inhibition of inflammation in osteoarthritis by triamcinolone acetonide released from a polyester amide microsphere platform
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Prolonged inhibition of inflammation in osteoarthritis by triamcinolone acetonide released from a polyester amide microsphere platform

机译：通过从聚酯酰胺微球平台释放的Triamcinolone丙酮酮长期抑制骨关节炎炎症

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Abstract Controlled biomaterial-based corticosteroid release might circumvent multiple injections and the accompanying risks, such as hormone imbalance and muscle weakness, in osteoarthritic (OA) patients. For this purpose, microspheres were prepared from an amino acid-based polyester amide (PEA) platform and loaded with triamcinolone acetonide (TAA). TAA loaded microspheres were shown to release TAA for over 60days in PBS. Furthermore, the bioactivity lasted at least 28days, demonstrated by a 80–95% inhibition of PGE2 production using TNFα-stimulated chondrocyte culture, indicating inhibition of inflammation. Microspheres loaded with the near infrared marker NIR780-iodide injected in healthy rat joints or joints with mild collagenase-induced OA showed retention of the microspheres up till 70days after injection. After intra-articular injection of TAA-loaded microspheres, TAA was detectable in the serum until day seven. Synovial inflammation was significantly lower in OA joints injected with TAA-loaded microspheres based on histological Krenn scores. Injection of TAA-loaded nor empty microspheres had no effect on cartilage integrity as determined by Mankin scoring. In conclusion, the PEA platform shows safety and efficacy upon intra-articular injection, and its extended degradation and release profiles compared to the currently used PLGA platforms may render it a good alternative. Even though further in vivo studies may need to address dosing and readout parameters such as pain, no effect on cartilage pathology was found and inflammation wa
机译：<！[cdata [ 抽象 基于对照的生物材料的皮质类固醇释放可能会绕过多次注射和随附的风险，如激素不平衡和肌肉弱点，如激素不平衡和肌肉弱点，在骨质节炎（OA）患者中。为此目的，从氨基酸基聚酯酰胺（豌豆）平台制备微球，并用抗菊氨酸酮（TaA）加载。显示TAA加载的微球以释放TAA超过60 天数。此外，生物活性持续至少28 天，所示的PGE 2 生产使用TNFα刺激的软骨细胞培养，表明炎症的抑制作用。用近红外标记NiR780-碘化物装载的微球注射在健康的大鼠关节或带温和胶原酶诱导的OA的关节中，显示微球至70 天注射后的含量。在关节内注射TAA加载的微球后，TAA在血清中可检测到七天。在基于组织学Krenn分数的基于组织学Krenn分数注入TAA负载的微球的OA关节中，滑膜炎症显着降低。通过人曼金得分确定的TAA负载或空的微球注射没有影响软骨完整性。总之，豌豆平台在关节内注射时显示安全性和功效，与目前使用的PLGA平台相比，其延长的降解和释放曲线可能使其成为一种良好的替代方案。即使进一步在体内：斜体>研究可能需要解决给药和读数参数，如疼痛，没有发现软骨病理学和炎症WA

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