Abstract：
Neuropathic pain is chronic pain caused by a lesion or disease of the somatosensory nervous system. Neuropathic pain, with a high incidence and complex pathogenesis, is one of the most significant areas of clinical medicine and basic research. Currently, prescribed treatments are still unsatisfactory or have limited effectiveness. A medicinal preparation is required that relieves the neuropathic pain and prolongs action time, which has not yet been discovered. In this study, MIL-101 (Fe) was employed as a drug carrier to regulate the release of diclofenac sodium, thereby achieving the effect of analgesia and sustained release. The release curves demonstrated that diclofenac sodium could be continuously released from MIL-101 (Fe) for more than 48 h. There was no toxicity in vitro and in vivo, and the safety of MIL-101 (Fe) was confirmed by hematoxylin and eosin as well as ELISA tests in vivo. The results of behavioral testing, pharmacokinetics, and RNA sequencing analysis showed that MIL-101 (Fe) loaded with diclofenac sodium could enhance the mechanical withdrawal threshold and alleviate cold allodynia induced by Spared Nerve Injury, prolonging the work time by three days. The results indicated that MIL-101 (Fe) exhibited excellent biocompatibility, while the MIL-101 (Fe)-DS demonstrated analgesic and controlled-release properties. These findings provide a scientific foundation for the clinical management of neuropathic pain and the development of a novel formulation.
摘要：
神经性疼痛是由体感神经系统的病变或疾病引起的慢性疼痛。神经性疼痛，发病率高，发病机制复杂，是临床医学和基础研究的重要领域之一。目前,处方治疗仍然不能令人满意或效果有限。需要一种减轻神经性疼痛并延长作用时间的药物制剂，尚未被发现。在这项研究中,以MIL-101(Fe)为药物载体调控双氯芬酸钠的释放,从而达到镇痛和缓释的效果。释放曲线表明，双氯芬酸钠可从MIL-101（Fe）中连续释放超过48h。MIL-101（Fe）的安全性通过苏木精和伊红以及体内ELISA测试得到证实。行为测试的结果，药代动力学，RNA测序分析表明,负载双氯芬酸钠的MIL-101(Fe)能提高机械戒断阈值,减轻备用神经损伤引起的冷异常性疼痛,将工作时间延长三天。结果表明,MIL-101(Fe)具有良好的生物相容性,而MIL-101（Fe）-DS表现出镇痛和控释特性。这些发现为神经性疼痛的临床管理和新型制剂的开发提供了科学依据。
