School of Ophthalmology & Optometry and Eye Hospital, Wenzhou Medical University, Wenzhou, PR China.
Institute of Biomaterials and Engineering, Wenzhou Medical University, Wenzhou, PR China.
Nanomedicine. 2018 Jan;14(1):185-193. doi: 10.1016/j.nano.2017.09.010. Epub 2017 Sep 29.
In the present study, we designed and synthesized a hydrogelator comprised of ibuprofen (IPF) and GFFY peptide linked through a cleavable ester bond. We found that the synthesized hydrogelator could spontaneously self-assemble into a hydrogel under a heating-cooling process. When the hydrogel was acted upon by an esterase, IPF was released in a sustained manner. Moreover, the hydrogel had significantly elevated anti-inflammatory efficacy, compared with IPF, in RAW264.7 macrophages. The hydrogel showed good cytocompatibility, as well as excellent ocular biocompatibility when instilled topically. In vivo results further demonstrated that the hydrogel had therapeutic efficacy comparable to that of a current treatment, sodium diclofenac (DIC) eyedrops, in suppressing ocular inflammation in lipopolysaccharide (LPS) induced uveitis. Our findings illustrated, for the first time, an effective approach for developing supramolecular assemblies as anti-inflammatory ophthalmic therapeutics for eye disorders.
在本研究中，我们设计并合成了一种由布洛芬（IPF）和 GFFY 肽通过可裂解的酯键连接而成的水凝胶剂。我们发现，所合成的水凝胶剂可以在加热-冷却过程中自发地自组装成水凝胶。当水凝胶受到酯酶作用时，IPF 以持续的方式释放。此外，与 IPF 相比，该水凝胶在 RAW264.7 巨噬细胞中表现出显著提高的抗炎功效。该水凝胶具有良好的细胞相容性，并且当局部滴注时具有极好的眼部生物相容性。体内结果进一步表明，该水凝胶在抑制脂多糖（LPS）诱导的葡萄膜炎中的眼部炎症方面具有与当前治疗方法（双氯芬酸钠（DIC）滴眼剂）相当的治疗效果。我们的研究结果首次阐明了一种有效的方法，用于开发作为眼部疾病抗炎治疗的超分子组装体。
