Drug-Bearing Supramolecular Filament Hydrogels as Anti-Inflammatory Agents,Theranostics

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Drug-Bearing Supramolecular Filament Hydrogels as Anti-Inflammatory Agents
Theranostics ( IF 12.4 ) Pub Date : 2017-05-12 , DOI: 10.7150/thno.19404
Zhipeng Chen _{1,

2,

3} , Lei Xing ₄ , Qin Fan _{1,

2} , Andrew G Cheetham ₃ , Ran Lin ₃ , Barbara Holt ₃ , Liwen Chen ₃ , Yanyu Xiao ₄ , Honggang Cui _{3,

5,

6}

Affiliation

We report here on the covalent conversion of the anti-inflammatory agent ketoprofen into self-assembling prodrugs that enable the effective purification of ketoprofen enantiomers, the improved selectivity and potency of ketoprofen, as well as the formation of one-component drug-bearing supramolecular hydrogels. We found that the ketoprofen hydrogelator could exhibit much-enhanced selectivity for cyclooxygenase 2 (COX-2) over COX-1, reduce the concentration of inflammatory cytokines (IL-1 and TNFα), and induce apoptosis in fibroblast-like synoviocytes while maintaining biocompatibility with healthy chondrocytes. In addition, these anti-inflammatory agent-containing hydrogels demonstrated the ability to retain the therapeutic within a joint cavity after intra-articular injection, exhibiting a slow, steady release into the plasma. We believe that upon further optimization these drug-based injectable supramolecular hydrogels could provide the basis for a local treatment strategy for rheumatoid arthritis and similar conditions.

中文翻译：

作为抗炎剂的载药超分子丝水凝胶

我们在此报告抗炎剂酮洛芬共价转化为自组装前药，从而能够有效纯化酮洛芬对映体，提高酮洛芬的选择性和效力，以及单组分载药超分子水凝胶的形成。我们发现酮洛芬水凝胶剂对环加氧酶 2 (COX-2) 的选择性比 COX-1 更高，降低炎症细胞因子（IL-1 和 TNFα）的浓度，并诱导成纤维样滑膜细胞凋亡，同时保持生物相容性与健康的软骨细胞。此外，这些含有抗炎剂的水凝胶表现出在关节内注射后将治疗剂保留在关节腔内的能力，并表现出缓慢、稳定的释放到血浆中的能力。我们相信，经过进一步优化，这些基于药物的可注射超分子水凝胶可以为类风湿关节炎和类似病症的局部治疗策略提供基础。

更新日期：2017-07-01

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