Self-assembly of a ibuprofen-peptide conjugate to suppress ocular inflammation

Abstract 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.