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

摘要: In the present study, we designed and synthesized a hydrogelator comprised of ibuprofen (IPF) GFFY peptide linked through cleavable ester bond. We found that could spontaneously self-assemble into hydrogel under heating-cooling process. When was acted upon by an esterase, IPF released in sustained manner. Moreover, had significantly elevated anti-inflammatory efficacy, compared with IPF, RAW264.7 macrophages. The showed good cytocompatibility, as well excellent ocular biocompatibility when instilled topically. vivo results further demonstrated therapeutic efficacy comparable to current treatment, sodium diclofenac (DIC) eyedrops, suppressing inflammation lipopolysaccharide (LPS) induced uveitis. Our findings illustrated, for first time, effective approach developing supramolecular assemblies ophthalmic therapeutics eye disorders.